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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T9685	DS-1971a	Sodium Channel	Membrane transporter/Ion channel
	DS-1971a 是选择性、口服有效的 NaV1.7抑制剂，对 hNaV1.7 和 mNaV1.7 的 IC50分别为 22.8 和 59.4 nM。DS-1971a 在缓解疼痛方面有研究价值。
T14984	CLP257	Potassium Channel	Membrane transporter/Ion channel
	CLP257 是有效的 K+-Cl- 协同转运蛋白 KCC2 选择性激活剂 (EC50: 616 nM)。它可减轻神经性疼痛大鼠的超敏反应，并在翻译后调节质膜 KCC2 蛋白周转。它在 KCC2 活性降低的神经元中恢复受损的 Cl- 转运。
T15050	Danicamtiv MYK-491,SAR 440181	Myosin	Cytoskeletal Signaling
	Danicamtiv (MYK-491) 是一种正性肌力药物，也是一种心肌肌球蛋白的选择性变构激活剂，可增加心脏收缩功能并保持机械效率。
T12051	MIV-247	Cysteine Protease	Proteases/Proteasome
	MIV-247 是一种具有选择性和高效性的 cathepsin S 抑制剂（人、小鼠和野猴 cathepsin S 的 Kis 分别为 2.1、4.2 和 7.5 nM），可减轻临床前神经性疼痛模型中的机械性异常性疼痛，可用于研究心肌损伤。
TP1309	Gastric mucin	Antibacterial; Antibiotic	Microbiology/Virology
	Gastric mucin 是一种能保护胃肠道免受酸、蛋白酶、致病微生物和机械创伤影响的糖蛋白。
TP1933	R715 TFA(185052-09-9 free base) R 715	Bradykinin Receptor	GPCR/G Protein
	R715 TFA(185052-09-9 free base) 是强效和选择性缓激肽 B1 受体拮抗剂 (pA2 = 8.49)。它对B2 受体无活性。它减少神经性疼痛小鼠模型中的机械性过度伤害感受。它代谢稳定。
T21380	Pravadoline WIN 48098-6,WIN48098-6,普拉朵林,WIN-48098-6	Cannabinoid Receptor	GPCR/G Protein
	Pravadoline (WIN48098-6) 是一种 cannabinoid 受体激动剂。 Pravadoline 抑制小鼠大脑中的 PGs 合成，并在受到各种热、化学和机械伤害性刺激的啮齿动物中显示出镇痛活性。
T11244	Etimizol Ethymisol,Ethimizole,Ethymisole	Others	Others
	Etimizol (Ethimizole) 对缺氧造成的失忆症有效果。
T0156	Rocuronium bromide ORG 9426,罗库溴铵,ORG 9426 (Bromide)	AChR	Neuroscience
	Rocuronium bromide (ORG 9426) 是一种氨基甾体类的、非去极化的神经肌肉受体抑制剂，也是一种肌肉松弛剂。
T77340L	AB21 HCl	Sigma receptor	GPCR/G Protein
	AB21 HCl 是 σ1 受体的选择性拮抗剂，σ1 受体的 Ki 为 13 nM，σ2 受体的 Ki 为 102 nM。 AB21 HCl 具有降低机械过敏的能力。
TP1220L	Carperitide acetate 醋酸卡培立肽,Carperitide acetate (89213-87-6 Free base),Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate	Endothelin Receptor	GPCR/G Protein
	Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate) 是一种由 28 个氨基酸组成的激素，由心脏产生并分泌，以响应心脏损伤和机械拉伸。Carperitide acetate 抑制内皮素-1 (endothelin-1) 分泌。
TP1904L	FSLLRY-NH2 TFA(245329-02-6 free base)	Protease-activated Receptor	GPCR/G Protein
	FSLLRY-NH2 TFA(245329-02-6 free base) 是一种蛋白酶激活受体 2 (PAR2) 抑制剂。在 ICR 小鼠中逆转紫杉醇诱导的机械异常性疼痛、热痛觉过敏和 PKC 激活。阻断分离的心脏成纤维细胞中的 ERK 活化和胶原蛋白生成。还可以减轻皮肤癣菌相关瘙痒小鼠模型的症状。
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。
T21543	AP 18	TRP/TRPV Channel	Membrane transporter/Ion channel
	AP-18 是选择性的 TRPA1 抑制剂。AP-18 可以抑制 50 μM 肉桂醛诱导的 TRPA1 激活，在小鼠和人中的 IC50 分别为 4.5 μM 和 3.1 μM。AP-18 可以逆转 CFA 诱导的小鼠机械性痛觉过敏。AP-18 可以浓度依赖的方式减弱 30 μM AITC 诱导的 Yo-Pro 摄取(IC50= 10.3 μM)。
T41005	PA-8	PACAP	GPCR/G Protein
	PA-8是一种小分子的的 PACAP I 型(PAC1)受体拮抗剂，有选择性、有效性和口服活性。PA-8抑制PACAP 诱导的CREB 在PAC1-受体上的磷酸化，但对VPAC11或VPAC2受体无抑制作用。PA-8也抑制pacap 诱导的体外cAMP 水平升高(IC50 = 2 nM)和体内鞘内注射后pacap 诱导的厌恶反应和机械异位性痛。
T80500	Jingzhaotoxin-X JZTX-X	Potassium Channel	Membrane transporter/Ion channel
	Jingzhaotoxin-X (JZTX-X) is a selective inhibitor of Kv4.2 and Kv4.3 potassium channels, inducing persistent mechanical hyperalgesia.
T15167	Draflazine R-75231	Others	Others
	Draflazine is an ENT1 inhibitor. It completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia. Draflazine also completely reverses the hypersensitivity of the carrageenan inflammation model of therma
T23642L	ADR-851 HCl Adr-851,Adr 851,Adr851
	ADR-851 HCl is an HT3 receptor antagonist. It works against mechanical, acute thermal, and formalin-induced inflammatory pain.
T11700	J-2156	Others	Others
	The ED50 of J-2156 in rats for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws was 3.7 and 8.0 mg/kg, respectively. J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC5
T40173	Spiropyran hexyl methacrylate
	Spiropyran hexyl methacrylate is a compound utilized to create a spiropyran-based polymeric hydrogel, specifically to enable light-activated mechanical actuation.
T25637	Laudexium methylsulfate Laudexium,Laudolissin methosulphate
	Laudexium methylsulfate is a neuromuscular blocking drug or skeletal muscle relaxant. It is used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.
TQ0002L	A-317491 sodium A-317491,A 317491,A317491
	A-317491 is an effective selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which reverses inflammatory mechanical hyperalgesia and relieves chronic inflammation and neuropathic pain in rats by acting on peripheral receptors.
T64113	J-2156 TFA
	J-2156 TFA 是一种选择性的、高效的生长抑素受体 4 型 (SST4) 激动剂，能够作用于人 SST4 受体 (IC50: 0.05 nM) 和大鼠 SST4 受体 (IC50: 0.07 nM)。J-2156 TFA 表现出抗炎活性，能够缓解大鼠同侧后爪的机械性异常性疼痛和机械性痛觉过敏。
T81231	S6 peptide
	S6 peptide, 作为一种潜在重要的核纤维层蛋白激酶，参与了机械负荷诱发的心肌肥厚过程并可被多种生长因子所激活。
T70340	JHU-58
	JHU-58 is a novel dipeptide MrgC agonist. JHU-58 inhibited both mechanical and heat hypersensitivity in rats after an L5 spinal nerve ligation (SNL). JHU58 attenuated the evoked excitatory postsynaptic currents in substantia gelatinosa (SG) neurons in wild-type mice, but not in Mrg knockout mice, after peripheral nerve injury.
T61091	p38-α MAPK-IN-4
	p38-α MAPK-IN-4 (Compound 69) 是一种选择性的p38α MAPK 抑制剂，IC50为 1.5 μM。p38-α MAPK-IN-4 在体内可快速、强烈地抑制机械性触诱发痛 (mechanical allodynia) 的发生。
TP1220	Carperitide Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
	Carperitide, a 28-amino acid hormone known as Atrial Natriuretic Peptide (ANP) (1-28), is naturally synthesized and released by the human heart in reaction to cardiac injury and mechanical stretch. This compound effectively suppresses endothelin-1 secretion in a dose-dependent manner.
T78916	AB21 oxalate	Sigma receptor	GPCR/G Protein
	AB21 oxalate为选择性S1R拮抗剂，对S1R的Ki为13 nM，对S2R为102 nM，能有效降低机械超敏反应。
TP1904	FSLLRY-NH2
	Selective PAR2 peptide antagonist. Reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice. Blocks ERK activation and collagen production in isolated cardiac fibroblasts. Also reduces symptoms in a mouse model of derm
T25636	Laudexium Laudexium ion,Laudexium cation
	Laudexium is a neuromuscular blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs. It is used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle re
T67212	Ligustrazine HCl
	Ligustrazine Hydrochloride, is a natural substance discovered in the plant Ligusticum chuanxiong Hort. It inhibits platelet aggregation, improves atherosclerosis situation, protects endothelium injury, and has antithrombotic effects.in vivo,ligustrazine hydrochloride at 10 and 20 mg/kg produced significant analgesic effects against mechanical stimuli,and ligustrazine hydrochloride at 80 mg/kg, also significantly alleviated cold hypersensitivity manifested by reduction in cold vocalization temper...
T78923	DDO-8926	Epigenetic Reader Domain	Chromatin/Epigenetic
	DDO-8926 是一种高效的选择性BET抑制剂，其通过抑制促炎细胞因子表达和降低神经兴奋性，显著减缓机械性超敏反应，被应用于神经性疼痛的研究领域。
T71559	Melanotan II acetate
	Melanotan II acetate is an agonist of melanocortin receptor 1 (MC1R), MC3R, MC4R, and MC5R. It has been shown to improve recovery of sciatic nerve function after mechanical injury and increase cisplatin-induced decreases in sensory nerve conduction velocity. Melanotan II acetate increases oxygen consumption and protein levels of uncoupling protein 1 (UCP1) in brown adipose tissue homogenates and decreases food intake, body weight, and serum levels of leptin, glucose, insulin, and cholesterol.
T76254	CD31
	CD31 (PECAM-1)，一种血小板内皮细胞粘附分子（platelet endothelial cell adhesion molecule-1），兼作产气荚膜梭菌b-Toxin (CPB) 的特异性内皮细胞受体。同时，CD31为ER-MP12抗原，桥接机械应力、代谢与炎症。其肽通过维持CD31 ITIM686与SHP2的磷酸化，抑制TCR诱导的T细胞激活。
T81664	NMB-1
	NMB-1，一种锥肽类似物，选择性抑制感觉神经元的持续机械激活电流(IC50: 1 μM)，有效抑制机械性疼痛，并可用于研究听力和压力诱发疼痛。
T35461	δ14-Triamcinolone acetonide
	δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide. Triamcinolone acetonide is a synthetic corticosteroid. It decreases cytokine levels, the firing rate of sensory neurons, and mechanical hypersensitivity in a rat spinal nerve ligation model when used at a dose of 1.5 mg/kg prior to and following surgery for three days. Triamcinolone acetonide also decreases outflow facility in a mouse model of steroid-induced glaucoma when 20 μl of a ...
T71955	C3001a
	C3001a is a selective activator for TREK, against other two-pore domain K+(K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mechanical allodynia and inflammation. C3001a represents a lead compound which could a...
T80446	ω-Conotoxin FVIA	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	ω-Conotoxin FVIA为N型钙离子通道(Cav2.2)的抑制剂，具有减轻尾神经损伤大鼠模型所诱导的机械性和热性异常疼痛的作用。该化合物在开发高效且低副作用止痛药物的研究中具有潜在应用价值。
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T38109	Galanin (2-11) amide (human, mouse, rat, porcine, bovine, ovine) (trifluoroacetate salt)
	Galanin (2-11) amide is a synthetic peptide fragment of the neuropeptide galanin and an agonist of the galanin-2 (GAL2) receptor (EC50= 9.32 nM in a fluorescence imaging plate reader assay).1It selectively binds to the GAL2receptor (IC50= 1.76 nM for the rat receptor) over the GAL1receptor (IC50= 879 nM for the human receptor) but does also bind to the GAL3receptor (Ki= 271 nM for the rat receptor).1,2Intracerebroventricular administration of galanin (2-11) amide (1 nmol/animal) decreases immobi...
T38147	(S)-AM1241 (S)-AM1241
	(S)-AM1241 binds to cannabinoid (CB) receptors and is selective for the CB2 over the CB1 receptor (Kis = 658 and >10,000 nM, respectively, in a membrane assay using human receptors). (S)-1241 acts as an agonist at human, rat, and mouse CB2 receptors but shows greater activity at human CB2 (EC50 = 131 nM) than at rat and mouse CB2 receptors (EC50 = 785 and 2,000 nM, respectively). Similar to the racemate AM1241 , (S)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. Th...
T76254L	CD31 TFA
	CD31 TFA（PECAM-1），血小板内皮细胞粘附分子（platelet endothelial cell adhesion molecule-1），是产气荚膜梭菌b-Toxin (CPB)内皮细胞特异性受体，亦为ER-MP12抗原，链接机械应力、代谢与炎症。该肽通过维持CD31 TFA ITIM686与SHP2的磷酸化，抑制TCR诱导的T细胞活化。
T38030	(R)-AM1241 (R)-AM1241
	(R)-AM1241 binds to cannabinoid (CB) receptors and has greater than 100-fold selectivity for the CB2 over the CB1 receptor (Kis = 15 and 5,000 nM, respectively, in a membrane assay using human receptors). (R)-AM1241 acts as an agonist at human CB2 receptors (EC50 = 118 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 315 and 341 nM, respectively). Similar to the racemate AM1241 , (R)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing...
T83701	TRPV1-Tat TFA Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat
	TRPV1-Tat是一种针对瞬时受体电位范烤苷1 (TRPV1) 的肽类拮抗剂。它由来自TRPV1的A-激酶锚蛋白(AKAP)结合域的736-745个氨基酸以及来自HIV Tat的细胞穿透肽序列组成。TRPV1-Tat (200 µM) 能够在使用初级小鼠背根神经节的整细胞膜片钳技术中抑制由热或棕榈酸酯12-肉豆蔻酸13-醋酸酯(PMA014)引起的电流。当以10或30 µM剂量给药时，它能增加大鼠后爪机械痛阈。
T35597	Neuromedin U-23 (rat) (trifluoroacetate salt)
	Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body ...
T83674	K 41498 TFA
	K 41498 是一种针对皮质酮释放因子受体2α（CRF2α）和CRF2β的肽拮抗剂，其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性，与CRF1相比（在表达人类受体的HEK293细胞中Ki值为425 nM）。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药，K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。
T83728	Tat-AKAP79 (326-336) TFA Tat-A-kinase Anchor Protein 79 (326-336)
	Tat-AKAP79 (326-336) 是一种肽，由HIV-1 Tat蛋白质转导域与对应于A-kinase anchor protein 79 (AKAP79) 326至336残基的11个氨基酸肽链相连组成。在200 µM浓度下，能抑制蛋白激酶A (PKA) 或PKC激活诱导的瞬时受体电位钒通道1 (TRPV1) 在分离的大鼠背根神经节 (DRG) 神经元中的敏感化。在体内，Tat-AKAP79 (326-336) 抑制小鼠由甲醛或phorbol 12-myristate 13-acetate (PMA014) 引发的伤害性行为。它还延长了小鼠对辐射热刺激爪子撤回的潜伏期，并在卡拉胶诱导的炎症性疼痛小鼠模型中增加了爪子撤回的机械阈力。
T36851	Peptide5
	Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain. O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 \|Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats....
T37718	Galanin (rat, mouse) (trifluoroacetate salt) GAL (rat, mouse),Galanin (rat, mouse) (trifluoroacetate salt)
	Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and...

化合物

Cat.No: T9685

Target: Sodium Channel

Cat.No: T14984

Target: Potassium Channel

Cat.No: T15050

Synonym: MYK-491,SAR 440181

Target: Myosin

Cat.No: T12051

Target: Cysteine Protease

Cat.No: TP1309

Target: Antibacterial, Antibiotic

R715 TFA(185052-09-9 free base)

Cat.No: TP1933

Synonym: R 715

Target: Bradykinin Receptor

Cat.No: T21380

Synonym: WIN 48098-6,WIN48098-6,普拉朵林,WIN-48098-6

Target: Cannabinoid Receptor

Cat.No: T11244

Synonym: Ethymisol,Ethimizole,Ethymisole

Target: Others

Rocuronium bromide

Cat.No: T0156

Synonym: ORG 9426,罗库溴铵,ORG 9426 (Bromide)

Target: AChR

Cat.No: T77340L

Target: Sigma receptor

Carperitide acetate

Cat.No: TP1220L

Synonym: 醋酸卡培立肽,Carperitide acetate (89213-87-6 Free base),Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate

Target: Endothelin Receptor

FSLLRY-NH2 TFA(245329-02-6 free base)

Cat.No: TP1904L

Target: Protease-activated Receptor

Cat.No: T14198

Target: GlyT

Cat.No: T21543

Target: TRP/TRPV Channel

Cat.No: T41005

Target: PACAP

Jingzhaotoxin-X

Cat.No: T80500

Synonym: JZTX-X

Target: Potassium Channel

Cat.No: T15167

Synonym: R-75231

Target: Others

Cat.No: T23642L

Synonym: Adr-851,Adr 851,Adr851

Cat.No: T11700

Target: Others

Spiropyran hexyl methacrylate

Cat.No: T40173

Laudexium methylsulfate

Cat.No: T25637

Synonym: Laudexium,Laudolissin methosulphate

A-317491 sodium

Cat.No: TQ0002L

Synonym: A-317491,A 317491,A317491

Cat.No: T64113

Cat.No: T81231

Cat.No: T70340

p38-α MAPK-IN-4

Cat.No: T61091

Cat.No: TP1220

Synonym: Atrial Natriuretic Peptide (ANP) (1-28), human, porcine

Cat.No: T78916

Target: Sigma receptor

Cat.No: TP1904

Cat.No: T25636

Synonym: Laudexium ion,Laudexium cation

Ligustrazine HCl

Cat.No: T67212

Cat.No: T78923

Target: Epigenetic Reader Domain

Melanotan II acetate

Cat.No: T71559

Cat.No: T76254

Cat.No: T81664

δ14-Triamcinolone acetonide

Cat.No: T35461

Cat.No: T71955

ω-Conotoxin FVIA

Cat.No: T80446

Target: Calcium Channel

Reduced Haloperidol

Cat.No: T37167

Galanin (2-11) amide (human, mouse, rat, porcine, bovine, ovine) (trifluoroacetate salt)

Cat.No: T38109

Cat.No: T38147

Synonym: (S)-AM1241

Cat.No: T76254L

Cat.No: T38030

Synonym: (R)-AM1241

Cat.No: T83701

Synonym: Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat

Neuromedin U-23 (rat) (trifluoroacetate salt)

Cat.No: T35597

Cat.No: T83674

Tat-AKAP79 (326-336) TFA

Cat.No: T83728

Synonym: Tat-A-kinase Anchor Protein 79 (326-336)

Cat.No: T36851

Galanin (rat, mouse) (trifluoroacetate salt)

Cat.No: T37718

Synonym: GAL (rat, mouse),Galanin (rat, mouse) (trifluoroacetate salt)

Cat. No.	Product Name	Target	Signaling Pathways
T80950	Tricetin 7-O-glucoside
	Tricetin 7-O-glucoside (compound 33)为一种黄酮类单-O-糖苷。

天然产物

Tricetin 7-O-glucoside

Cat.No: T80950

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