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71

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9625	Sandalore	Apoptosis	Apoptosis
	Sandalore 通过减少细胞凋亡和增加外根鞘中延长生长期的生长因子 IGF-1 的产生来延长人类头发的生长。 Sandalore 是嗅觉受体 OR2AT4 的选择性激动剂。
T3635	IQ 1 IQ1,IQ-1	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	IQ 1 有多种作用，如保持小鼠ESCs 的多功能性、降低Wnt 刺激的磷酸化、阻止PP2A/Nkd 的相互作用等等。
T7556	Fadrozole hydrochloride CGS 16949A,盐酸法倔唑	Aromatase	Endocrinology/Hormones
	Fadrozole hydrochloride (CGS 16949A) 是一种选择性的、有效，和非甾体类的芳香化酶抑制剂(IC50:6.4 nM)。
T39308	Boc-Asp(OMe)-fluoromethyl ketone Boc-Asp(OMe)-fluoromethyl ketone,Boc-Asp(OMe)-FMK	Caspase	Apoptosis; Proteases/Proteasome
	Boc-Asp(OMe)-fluoromethyl ketone (Boc-Asp(OMe)-FMK) 是广谱的 caspase 抑制剂，可抑制 Fas 介导的吞噬作用和氧化破裂抑制，但对 IL-8 的趋化活性无影响。
T20968	CyPPA	Potassium Channel; Dopamine Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	CyPPA 是hSK2和hSK3的阳性调节剂，其EC50值分别为 5.6 μM 和14 μM。它对 hSK1 和 hIK 通道无活性。
T23563	ZM 226600	Potassium Channel	Membrane transporter/Ion channel
	ZM 226600是一种 ATP 敏感的钾通道开启剂，EC50值是500 nM。ZM226600 对膀胱自发活动有抑制作用。
T35033	Vamicamide FK 176,FK-176,FK176	AChE	Neuroscience
	Vamicamide (FK 176)是一种新型抗胆碱能化合物。Vamicamide 在 32 mg/kg （p.o.）或更高时增加小鼠的自发运动活动，并在 100 mg/kg 时抑制小鼠强直性惊厥。
T12255	NS19504	Potassium Channel	Membrane transporter/Ion channel
	NS19504 是 Ca2+激活的 K+通道激活剂 (EC50=11.0 µM)，对膀胱平滑肌自发性相位收缩具有松弛作用。
TP1526L1	Fibronectin CS1 Peptide acetate	Others	Others
	Fibronectin CS1 Peptide acetate 存在于 III 型同源连接段 (IIICS) 以及 C-274（细胞结合结构域）中。 Fibronectin CS1 Peptide 缺乏含有 Arg-Gly-Asp 的结构域，在自发和实验性转移模型中积极抑制肿瘤转移。
T35033L	(S)-Vamicamide (S)-Vamicamide (Iso-132373-81-0)	AChE	Neuroscience
	(S)-Vamicamide 是一种新型抗抗胆碱能化合物。Vamicamide 在 32 mg/kg 或更高（p.o.）时增加小鼠的自发运动活动，并在 100 mg/kg 时抑制小鼠强直性惊厥。
T14569	BI8626	E1/E2/E3 Enzyme	Ubiquitination
	BI8626 是一种泛素连接酶 HUWE1 抑制剂，对 NOD/ShiLtj 小鼠自发性干燥综合征具有保护作用。BI8626 抑制细胞内胆固醇并降低磷酸化 ZAP-70、CD25 和其他激活标志物的表达，抑制 CD4 T 细胞的增殖。
T10893	CS-722 Free base	Others	Others
	CS-722 Free base是一种合成的中枢作用肌肉松弛剂，它展现出肌肉松弛效果并抑制脊髓反射。可能通过限制钠和钙流动，从而在海马培养物中减少自发的抑制性和兴奋性突触后电流。
TP1940L1	Ac-RYYRIK-NH2 acetate	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Ac-RYYRIK-NH2 acetate 是 nociceptin/orphanin FQ(noc/OFQ) 受体的激动剂，影响自发运动活动。它是转染在 CHO 细胞中的 ORL1 的部分激动剂，可拮抗大鼠脑膜和切片中 noc/OFQ 对 [35S]-GTPgammaS 与 G 蛋白结合的刺激。
T4132	BPTU BMS-646786	P2Y Receptor	GPCR/G Protein; Neuroscience
	BPTU (BMS-646786) 是一种非核苷酸类P2Y1受体变构拮抗剂，能够阻断位于胃肠道神经肌肉接头的 P2Y1受体，具有抗血栓活性。
T22171	WWL123	MAGL	Metabolism
	WWL123 是一种有效的选择性 ABHD6 抑制剂，IC50 为 430 nM。WWL123 可穿过血脑屏障并抑制脑实质中的 ABHD6。WWL123 阻断 ABHD6 在 Pentylenetetrazole (PTZ)诱导的 R6/2 小鼠癫痫样发作和自发性癫痫发作中发挥抗癫痫作用。
T77599	Methyl retinoate Retinoic acid, methyl ester	Others	Others
	Methyl retinoate (Retinoic acid, methyl ester) 在体内实验中会诱导给部位发生无菌炎症，会使血液中白细胞数量增加，而红细胞和Hb含量减少。Methyl retinoate 可促进自发性白血病的产生。Methyl retinoate 可用于治疗因维生素A缺乏而产生的胃肥大和溃疡。
T14198	ALX-1393	GlyT	Neuroscience
	ALX-1393 是一种选择性 GlyT2 抑制剂，通过浓度依赖性的方式有效地降低了神经元动作电位的活性，抑制自发网络通过在脊髓腹角诱导甘氨酸能强直电流的活动。对大鼠急性疼痛模型中的热，机械和化学刺激具有抗伤害作用。
T37807	JTV 519 fumarate
	Ryanodine receptor (RyR) inhibitor; stabilizes RyR2 in a closed conformation. Exhibits antiarrhythmic and cardioprotective properties in vivo. Hunt et al (2007) K201 (JTV519) suppresses spontaneous Ca2+ release and [3H]ryanodine binding to RyR2 irrespective of FKBP12.6 association. Biochem.J. 404 431 PMID:17313373 \|Chen et al (2008) Effect of K201, a novel antiarrhythmic drug on calcium handling and arrhythmogenic activity of pulmonary vein cardiomyocytes. Br.J.Pharmacol. 153 915 PMID:17994112 \|...
T0866	Propafenone Rythmol,普罗帕酮,Propafenonum	Potassium Channel; MRP; Sodium Channel	Immunology/Inflammation; Membrane transporter/Ion channel
	Propafenone (Propafenonum) 是钠通道阻滞剂，它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ，具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡，从而抑制食管癌增殖。
T27874	LY 135305 LY-135305,LY135305
	LY 135305 is a inhibition of spontaneous metastasis.
TP2480	Locustamyotropin Lom-MT,Locustamyotropin I,Lom MT,LomMT,Gly-ala-val-pro-ala-ala-gln-phe-ser-pro-arg-leu-NH2
	Locustamyotropin is a novel peptide isolated from Leucophae maderae; stimulates the spontaneous contractions of the hindgut of Leucophaea maderae.
T15449	GW-406381	COX	Immunology/Inflammation; Neuroscience
	GW406381 is a highly selective inhibitor of cyclooxygenase-2 (COX-2). GW406381 also attenuates spontaneous ectopic discharge in the sural nerves of rats following chronic constriction injury.
T26614	Ambucetamide Bersen,Meritin,Dibutamid
	Ambucetamide is an antispasmodic, it may inhibit or diminish the spontaneous rhythmical activity of the human myometrium.
T23739	Antho-riamide I
	Antho-Riamide I is an active peptide. It also inhibits the spontaneous contraction of sea anemone muscles.
T71733	VU0606170
	VU0606170 is a slack channels inhibitor and was shown to successfully decrease the malfunctioning spontaneous firing rate of cortical neurons, providing a potential avenue for achieving an anti-epileptic effect not previously attainable.
T19737	Perthane
	Perthane is the diethyl derivative of common pesticide DDD. It may cause adrenocortical atrophy in humans,and also prevent the formation of spontaneous mammary carcinoma.
T30460	BIR2 Balloon inducing reagent 2,BIR-2,BIR 2,Balloon inducing reagent-2
	BIR2 is a balloon inducing reagent, which triggers a spontaneous self-organization process, leading to the formation of 3-D balloon like structure during hESC differentiation.
T30459	BIR1 Balloon inducing reagent-1,Balloon inducing reagent 1
	BIR1 is a balloon inducing reagent, which triggers a spontaneous self-organization process, leading to the formation of 3-D balloon like structure during hESC differentiation.
T70151	MeTC7
	MeTC7 is a VDR antagonist, which can be synthesized from 7-dehydrocholesterol (6) in two steps, inhibits VDR selectively, suppresses the viability of cancer cell-lines, and reduces the growth of the spontaneous transgenic TH-MYCN neuroblastoma and xenografts in vivo.
T70214	BMS-986202
	BMS-986202 is a novel Tyk2 inhibitor, binding to Tyk2 JH2, showing efficacies for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.
T71854	AA43279
	AA43279 is a novel selective Nav1.1 activator, increasing the firing activity of parvalbumin-expressing, fast-spiking GABAergic interneurons and increasing the spontaneous inhibitory post-synaptic currents (sIPSCs) recorded from pyramidal neurons.
T69324	Clofeverine hydrochloride
	Clofeverine hydrochloride is the salt form of Clofeverine (free base), a highly selective relaxant for gastrointestinal smooth muscles with a beta-receptor stimulative nature. On isolated ileum, the inhibitory effect of clofeverine for spontaneous motility was comparable to that of isoproterenol and 100 times higher than that of papaverine.
T37319	5β-Dihydroprogesterone
	5β-Dihydroprogesterone (5β-DHP) is a progesterone receptor agonist and metabolite of progesterone .1,2It is formed from progesterone by 5β-reductase.25β-DHP inhibits spontaneous contractions in isolated rat uterus when used at a concentration of 10 μg/ml, an effect that can be blocked by the progesterone receptor antagonist RU486 but not the GABAAreceptor antagonist picrotoxin .1It is a negative modulator of homooligomeric Ρ1 subunit-containing GABAAreceptors, inhibiting GABA-induced currents in...
T78289	Ligelizumab QGE 031,Anti-IGHE Recombinant Antibody
	Ligelizumab (QGE 031)为一种针对慢性自发性荨麻疹研究的人源化高亲和性抗IgE单克隆抗体。
T69073	COTC
	COTC is a bacterial metabolite that has anticancer activity and inhibits glyoxalase in the presence of glutathione (GSH) and the proliferation of HeLa cells, as well as reduces tumor growth and improves survival in an Ehrlich murine spontaneous adenocarcinoma model.
T28898	T145 T 145,T-145
	T145 inhibits growth of Enterococcus faecalis, Staphylococcus aureus and Mycobacterium tuberculosis (Mtb) with sub μg/ml potencies that are potentially therapeutically valuable. T145 minimizes selection of spontaneous resistant mutants, a trait that prolo
T69126	Clofeverine (free base)
	Clofeverine (free base) is a highly selective relaxant for gastrointestinal smooth muscles with a beta-receptor stimulative nature. On isolated ileum, the inhibitory effect of clofeverine for spontaneous motility was comparable to that of isoproterenol and 100 times higher than that of papaverine.
T21921	Valeroyl Salicylate 2-Valeryloxybenzoic acid,戊酰基水杨酸	Others	Others
	Valeroyl Salicylate (2-Valeryloxybenzoic acid) 具有抗炎作用，可延长寿命，延缓随年龄增长而导致的自发活动下降，并提高抗压能力。
T38172	RO 5263397 hydrochloride
	Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 \|Galley et al (2015) Discovery ...
T80908	Tyrosylhistidine
	Tyrosylhistidine是由酪氨酸和组氨酸构成的二肽(Tyr-His)。作为一种口服降血压肽，它能够降低自发性高血压模型小鼠的血压。
T21927	A 61603 hydrobromide
	A-61603 是一种选择性的α1A 肾上腺素能受体激动剂。A-61603 在体外增加大鼠心室肌细胞自发性钙瞬变的频率。
T39936	HM Janelia Fluor® 526, SE HM-JF526 NHS
	HM Janelia Fluor 526, SE (HM-JF526 NHS) is a derivative of hydroxymethyl JF526 (HM-JF526). SMLM (single-molecule localization microscopy) imaging in standard phosphate-buffered saline (pH 7.4) revealed that the HM-JF526 label showed spontaneous blinking behavior throughout the imaging session and did not require short-wavelength activation light.
T26665	AS604872 AS-604872,AS 604872
	AS604872 is a selective antagonist of the FP receptor.. AS604872 significantly accelerated degeneration of the media in both cerebral artery and aorta as evidenced by thinning of the media and disruption of the elastic lamina and promoted IA and aortic di
T38221	N,N-Dipropyldopamine (hydrobromide)
	N,N-Dipropyldopamine is a dopamine receptor agonist.1,2,3 It decreases dihydrophenylalanine (DOPA) levels in the limbic forebrain and striatum of reserpinized rats (ED50s = 25 and 20 μmol/kg, respectively), as well as reduces homovanillic acid levels in rat striatum when administered at a dose of 80 μmol/kg.1 N,N-Dipropyldopamine (0.5-16 mg/kg) reduces spontaneous locomotor activity in mice, an effect that can be reversed by the antipsychotic spiroperidol.2,3
T70896	PF05020182
	PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in cont...
T71426	STA-1474
	STA-1474 is a water soluble prodrug of ganetespib (formerly STA-9090). STA-1474 will metabolized to Ganetespib, which is a potent HSP90 inhibitor previously shown to kill canine tumor cell lines in vitro and inhibit tumor growth in the setting of murine xenografts. The purpose of the following study was to extend these observations and investigate the safety and efficacy of STA-1474 in dogs with spontaneous tumors.
T29002	Trazium Esilate EGYT3615,EGYT-3615,EGYT 3615
	Trazium esilate is an adrenergic receptor antagonist. Trazium esilate is a weak displacer on a1-, a2- and D2-receptors, however, it induced a2-receptor desenzitization after repeated treatment. It had no influence on rat brain cortical noradrenaline and s
T36218	19R(20S)-EpDPA
	19R(20S)-EpDPA is an oxylipin and a metabolite of docosahexaenoic acid .1,2It is formed from DHA by various cytochrome P450 (CYP) isoforms in a stereoselective manner.219R(20S)-EpDPA (30 nM) prevents calcium-induced increases in the spontaneous beating of isolated neonatal rat cardiomyocytes (NRCMs).3 1.Cinelli, M.A., Yang, J., Scharmen, A., et al.Enzymatic synthesis and chemical inversion provide both enantiomers of bioactive epoxydocosapentaenoic acidsJ. Lipid Res.59(11)2237-2252(2018) 2.Lucas...
T73756	Galactonic acid
	Galactonic acid 是半乳糖代谢中的一种糖酸，通过半乳糖脱氢酶作用，半乳糖转化为半乳糖内酯，随后经自发或酶催化反应转化为 Galactonic acid。
T35993	Epitalon (acetate)
	Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w/w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg/animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatoni...

化合物

Cat.No: T9625

Target: Apoptosis

Cat.No: T3635

Synonym: IQ1,IQ-1

Target: Wnt/beta-catenin

Fadrozole hydrochloride

Cat.No: T7556

Synonym: CGS 16949A,盐酸法倔唑

Target: Aromatase

Boc-Asp(OMe)-fluoromethyl ketone

Cat.No: T39308

Synonym: Boc-Asp(OMe)-fluoromethyl ketone,Boc-Asp(OMe)-FMK

Target: Caspase

Cat.No: T20968

Target: Potassium Channel, Dopamine Receptor

Cat.No: T23563

Target: Potassium Channel

Cat.No: T35033

Synonym: FK 176,FK-176,FK176

Target: AChE

Cat.No: T12255

Target: Potassium Channel

Fibronectin CS1 Peptide acetate

Cat.No: TP1526L1

Target: Others

Cat.No: T35033L

Synonym: (S)-Vamicamide (Iso-132373-81-0)

Target: AChE

Cat.No: T14569

Target: E1/E2/E3 Enzyme

CS-722 Free base

Cat.No: T10893

Target: Others

Ac-RYYRIK-NH2 acetate

Cat.No: TP1940L1

Target: Opioid Receptor

Cat.No: T4132

Synonym: BMS-646786

Target: P2Y Receptor

Cat.No: T22171

Target: MAGL

Methyl retinoate

Cat.No: T77599

Synonym: Retinoic acid, methyl ester

Target: Others

Cat.No: T14198

Target: GlyT

JTV 519 fumarate

Cat.No: T37807

Cat.No: T0866

Synonym: Rythmol,普罗帕酮,Propafenonum

Target: Potassium Channel, MRP, Sodium Channel

Cat.No: T27874

Synonym: LY-135305,LY135305

Locustamyotropin

Cat.No: TP2480

Synonym: Lom-MT,Locustamyotropin I,Lom MT,LomMT,Gly-ala-val-pro-ala-ala-gln-phe-ser-pro-arg-leu-NH2

Cat.No: T15449

Target: COX

Cat.No: T26614

Synonym: Bersen,Meritin,Dibutamid

Antho-riamide I

Cat.No: T23739

Cat.No: T71733

Cat.No: T19737

Cat.No: T30460

Synonym: Balloon inducing reagent 2,BIR-2,BIR 2,Balloon inducing reagent-2

Cat.No: T30459

Synonym: Balloon inducing reagent-1,Balloon inducing reagent 1

Cat.No: T70151

Cat.No: T70214

Cat.No: T71854

Clofeverine hydrochloride

Cat.No: T69324

5β-Dihydroprogesterone

Cat.No: T37319

Cat.No: T78289

Synonym: QGE 031,Anti-IGHE Recombinant Antibody

Cat.No: T69073

Cat.No: T28898

Synonym: T 145,T-145

Clofeverine (free base)

Cat.No: T69126

Valeroyl Salicylate

Cat.No: T21921

Synonym: 2-Valeryloxybenzoic acid,戊酰基水杨酸

Target: Others

RO 5263397 hydrochloride

Cat.No: T38172

Tyrosylhistidine

Cat.No: T80908

A 61603 hydrobromide

Cat.No: T21927

HM Janelia Fluor® 526, SE

Cat.No: T39936

Synonym: HM-JF526 NHS

Cat.No: T26665

Synonym: AS-604872,AS 604872

N,N-Dipropyldopamine (hydrobromide)

Cat.No: T38221

Cat.No: T70896

Cat.No: T71426

Trazium Esilate

Cat.No: T29002

Synonym: EGYT3615,EGYT-3615,EGYT 3615

Cat.No: T36218

Galactonic acid

Cat.No: T73756

Epitalon (acetate)

Cat.No: T35993

Cat. No.	Product Name	Target	Signaling Pathways
TN1698	Glucotropaeolin potassium 金莲葡糖硫苷钾盐,Glucotropaeolin,Benzylglucosinolate potassium,Glucotropaeolin Potassium Salt	Others	Others
	Glucotropaeolin potassium (Benzylglucosinolate potassium) 存在于十字花科蔬菜中，并且可适度减少动物的自发性DNA 损伤。
T4S1518	Pseudoginsenoside RT1 拟人参皂苷 RT1,假人参皂苷RT1	Others	Others
	Pseudoginsenoside RT1 是分离自 Randia siamensis 中，具有鱼毒素作用。它可导致血压下降、心率加快和子宫自发收缩力增加。
T4890	3-Nitro-L-tyrosine 3-Nitrotyrosine,3-硝基-L-酪氨酸	Endogenous Metabolite	Metabolism
	3-Nitro-L-tyrosine (3-Nitrotyrosine) 在系统自免疫原性条件下，能够作无氮自由基修饰蛋白的生物标记物。
T8716	physalin F 酸浆苦味素F,酸浆苦素 F	Apoptosis	Apoptosis
	Physalin F 是一种分泌型甾体，诱导人外周血单个核细胞凋亡，降低人 T 淋巴细胞 1 型病毒感染后的自发增殖和细胞因子的产生，具有强烈抗炎和免疫调节作用。
T2S1727	Lycorenine	Antifection	Microbiology/Virology
	Lycorenine may produce a decrease in blood pressure as the result of alpha-adrenergic blockade in conjunction with the reduction of the spontaneous sympathetic nerve activity, and produce bradycardia by modifying vagal activity. The development of tachyph
TN4519	Mesuaxanthone A 胡桐，海棠木	Others	Others
	Mesuaxanthone A and mesuaxanthone B are two yellow pigments.They produce varying degrees of C.N.S. depression characterised by ptosis, sedation, decreased spontaneous motor activity, loss of muscle tone, potentiation of pentobarbitone sleeping time and et
T83916	Cytogenin
	Cytogenin（一种源自S. eurocidicum的香豆素衍生物）具有多种生物活性。在每日给药25 mg/kg剂量下，能减轻Ehrlich鼠自发性腺癌模型的肿瘤重量。在体内，Cytogenin（每日30和100 mg/kg）可减少链脲佐菌素诱导的体重下降和血浆葡萄糖水平上升，以及小鼠糖尿病模型中巨噬细胞胰腺浸润。同时，在每日100 mg/kg的剂量下，能降低小鼠巨噬细胞中zymosan和LPS诱导的一氧化氮产生，及LPS诱导的Il-6水平增加。

天然产物

Glucotropaeolin potassium

Cat.No: TN1698

Synonym: 金莲葡糖硫苷钾盐,Glucotropaeolin,Benzylglucosinolate potassium,Glucotropaeolin Potassium Salt

Target: Others

Pseudoginsenoside RT1

Cat.No: T4S1518

Synonym: 拟人参皂苷 RT1,假人参皂苷RT1

Target: Others

3-Nitro-L-tyrosine

Cat.No: T4890

Synonym: 3-Nitrotyrosine,3-硝基-L-酪氨酸

Target: Endogenous Metabolite

Cat.No: T8716

Synonym: 酸浆苦味素F,酸浆苦素 F

Target: Apoptosis

Cat.No: T2S1727

Target: Antifection

Mesuaxanthone A

Cat.No: TN4519

Synonym: 胡桐，海棠木

Target: Others

Cat.No: T83916

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