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Search Results for " paw "

34

抑制剂 & 化合物

13

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T10466	BAY-1797	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	BAY-1797 是具有口服活性的选择性P2X4高效拮抗剂，对人 P2X4 的IC50为 211 nM，具有抗伤害和抗炎作用。
T9216	MLT-943 MLT943	MALT	Immunology/Inflammation
	ML-943 是选择性的、口服活性的MALT1 protease 抑制剂。它可抑制 PBMC 或全血中 IL-2 的分泌，PBMC 中抑制的IC50值为 0.07~0.09 μM，全血中抑制的IC50值为 0.6~0.8 μM)。它具有抗炎作用，可用于研究 FcgR 介导的炎症。
T36534	SDZ 224-015 SDZ 224015	IL Receptor; Caspase	Apoptosis; Immunology/Inflammation; Proteases/Proteasome
	SDZ 224-015 是白细胞介素-1β（IL-1β）转化酶和 Caspase-1 的口服活性抑制剂。SDZ 224-015 具有抗 COVID-19 和抗炎活性，可减少角叉菜胶诱导的大鼠爪子水肿。
T36619	Aligeron	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Aligeron 是一种非选择性的prostaglandin (PG)拮抗剂，对PGF2α和PGE2诱导的猫血压下降有抑制作用，可用于抑制PGF2α诱导的小鼠腹泻和PGE2诱导的大鼠爪水肿。Aligeron 对血管并发症具有抗氧化保护作用。
T68025	Zoliprofen	Others	Others
	Zoliprofen 是一种一种高效的且可口服的非甾体抗炎剂，具有抗炎、解热和镇痛活性，对角叉菜素、制霉菌素、刀豆球蛋白A 诱导的大鼠爪水肿，以及抗大鼠兔血清诱导的骨折或背皮水肿具有抑制作用。Zoliprofen 在大鼠和兔子中对胶原蛋白或花生四烯酸引起的血小板聚集方面比布洛芬和非诺洛芬有效20倍。Zoliprofen 对小鼠内毒素诱导的腹泻和花生四烯酸诱导的兔急性死亡抑制作用显著。
T70618	SK609
	SK609 is a selective dopamine D3 receptor agonist which significantly improves the performance of the impaired paw and normalizes the bilateral asymmetry associated with the hemiparkinson rat.
T24950	VUF-10214 VUF 10214,VUF10214
	VUF-10214 is an H4 receptor-ligand. VUF-10214 has significant anti-inflammatory properties in the carrageenan-induced paw edema model in vivo studies in the rat reveal.
T27752	KT109 KT-109,KT 109
	KT109 is a selective inhibitor of DAGLβ (IC50 = 42 nM). KT109-treated wild-type mice displayed reductions in LPS-induced allodyni as well as in DAGL-β (-/-) micea. Repeated KT109 administration prevented the expression of LPS-induced allodynia, without ev
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...
T78967	Anti-inflammatory agent 40	Parasite	Microbiology/Virology
	Anti-inflammatory agent 40 是潜在的口服抗疟疾(anti-malarial)与抗炎(Anti-inflammatory)化合物，能抑制卡拉胶诱导的足跖肿胀。
T37156	8(S),15(S)-DiHETE
	8(S),15(S)-DiHETE is formed when 15(S)-HETE is subjected to further oxidation by 15-LO. It causes eosinophil chemotaxis with an ED50 value of 1.5 μM but is not chemotactic for neutrophils. 8(S),15(S)-DiHETE antagonizes the hyperalgesic activity of 8(R),15(S)-DiHETE and LTB4 in the rat hind paw pain model.
T38209	Hodgkinsine
	Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 5 mg/kg. 1.Amador, T.A., Verotta, L., Nunes, D.S., et al.Antinociceptive profile of hodgkinsinePlanta Med.66(8)770-772(2000)
T38327	Cryogenine
	Cryogenine is an alkaloid originally isolated from H. salicifolia that has anti-inflammatory activity.1 It inhibits prostaglandin synthetase (IC50 = 424 μM). Cryogenine (100 mg/kg per day, p.o.) reduces paw edema and the mean arthritic index in a rat model of adjuvant-induced polyarthritis.2 \|1. Lema, W.J., Blankenship, J.W., and Malone, M.H. Prostaglandin synthetase inhibition by alkaloids of Heimia salicifolia. J. Ethnopharmacol. 15(2), 161-167 (1986).\|2. Kosersky, D.S., Brown, J.K., and Malon...
T83048	Anti-inflammatory agent 64	ROS Kinase	Tyrosine Kinase/Adaptors
	Anti-inflammatory agent 64（compound 4b）能抑制IL-6和TNF-α的分泌，具备抗氧化及抗炎活性，无论在体内外均有效，能显著减轻足跖水肿。
T75954	Mambalgin 1 TFA
	Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.
T68393	SNX-7081
	NX-7081 is a novel small molecule inhibitor of Hsp90, which blocks components of inflammation, including cytokine production, protein kinase activity, and angiogenic signaling. SNX-7081 showed strong binding affinity to Hsp90 and expected induction of Hsp70. NF-kappaB nuclear translocation was blocked by SNX-7081 at nanomolar concentrations, and cytokine production was potently inhibited. Growth factor activation of ERK and JNK signaling was significantly reduced by SNX-7081. NO production was a...
T36101	Psychotridine
	Psychotridine is an alkaloid that has been found inP. forsterianaand has diverse biological activities.1,2,3It inhibits ADP-, collagen-, or thrombin-induced aggregation of washed isolated human platelets with IC50values of 1.4, 1.4, and 3.9 μM, respectively.1Psychotridine (2.5 or 5 μM) is cytotoxic to HTC rat hepatocellular carcinoma cells.2It reduces paw licking induced by capsaicin in mice when administered at doses of 0.5, 2.5, or 5 mg/kg.3 1.Beretz, A., Roth-Georger, A., Corre, G., et al.Pol...
TP1408	Peptide 401
	Peptide 401 is an antimicrobial peptide (AMP) derived from the venom of bees and wasps. Peptide 401 induces mast cell degranulation, activating histamine release from peritoneal mast cells. Additionally, peptide 401 exhibits some anti-inflammatory activit
T69451	R-130823
	R-130823 is a ighly selective inhibition against mitogen-activated protein kinase p38alpha (IC50=22 nM). The release of tumor necrosis factor-alpha, interleukin-1beta, -6 and -8 was inhibited in lipopolysaccharide-stimulated human blood pretreated by R-130823 , with IC50 values of 0.089, 0.066, 0.95 and 0.16 microM, respectively. R-130823 reduced the established hind paw swelling in rat adjuvant-induced arthritis, while methotrexate showed no suppression. In the same model, R-130823 ameliorated ...
T36064	N-Oleoyl Glutamine
	N-Oleoyl glutamine is an endogenous N-acyl amine.1,2It is both formed and degraded by peptidase M20 domain-containing 1 (PM20D1), a factor secreted by thermogenic adipose cells. N-Oleoyl glutamine (50 μM) induces mitochondrial uncoupling to increase respiration in C2C12 cells by 64%.3It inhibits capsaicin-induced calcium flux in HEK293A cells co-transfected with transient receptor potential vanilloid 1 (TRPV1) and red fluorescent protein (RFP).2N-Oleoyl glutamine (100 mg/kg) reduces the number o...
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 ...
TP2003	Mambalgin 1
	Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases late
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。
T37182	AX 048
	The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes. AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of r...
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。
T83143	Alloferon 1
	Alloferon 1 是一种具有抗病毒和抗肿瘤功能的肽。它能激活人外周血淋巴细胞的天然细胞毒性，诱导IFN合成，并在小鼠体内增强其抗病毒和抗肿瘤的防御机制。此外，Alloferon 1 在 λ-角叉菜胶诱导的足水肿模型中展现出抗炎作用。它可从双翅目昆虫丽蝇Calliphora vicina的血液中提取。
T71212	Lornoxicam-d4
	Lornoxicam-d4 is intended for use as an internal standard for the quantification of lornoxicam by GC- or LC-MS. Lornoxicam is a COX inhibitor and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic properties. It inhibits production of thromboxane B2 from arachidonic acid in HEL human erythroleukemic cells, which endogenously express COX-1, as well as inhibits LPS-induced formation of prostaglandin F1α from arachidonic acid in Mono-Mac-6 cells, which endogenously e...
T37127	L-AP4 monohydrate L-AP4 monohydrate
	L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunctio...
T38110	Galanin (Human) (Acetate)
	Galanin (Human) (Acetate)是一种含有30个氨基酸的神经肽和丙氨酸(GAL)受体激动剂。在表达重组人gal1受体的HEK293E 细胞(EC50= 0.031 nM)中，它抑制佛司可林诱导的cAMP 产生，并刺激表达重组人gal2受体的CHO 细胞(EC50= 12.3 nM)中肌醇磷酸的积累。Galanin (Human) (Acetate)诱导离体大鼠纵向眼底收缩，ec50值为13.8 nM。在大鼠福尔马林试验的第二阶段，鞘内给药人甘丙肽(3、10和30 nmol/只)可减少大鼠舔爪和退缩。
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...
T83875	HUP-55
	HUP-55是一种脯氨酸内肽酶的抑制剂（IC50 = 5 nM）。在10 µM的浓度下，它可减少Neuro2a细胞中α-突触核蛋白二聚体的形成，促使HEK293细胞发生自噬，并降低SH-SY5Y细胞中由过氧化氢诱导的反应性氧种（ROS）产量的增加。此外，HUP-55（10 mg/kg）在通过腺病毒递送α-突触核蛋白编码载体（AAV-αSyn）诱导的帕金森病小鼠模型中，能减少患侧爪的使用和纹状体中寡聚体α-突触核蛋白水平。
T83732	Tat-CBD3A6K TFA
	Tat-CBD3A6K是一种肽类化合物，为N型电压门控钙通道Cav2.2以及collapsin response mediator protein 2 (CRMP2) 蛋白-蛋白相互作用抑制剂Tat-CBD3的衍生物。Tat-CBD3A6K (10 mg/kg) 能够阻止由d4T (stavudine)引发的大鼠抗逆转录病毒神经病痛模型中爪撤回阈值的下降，并减少同一大鼠分离的背根神经节(DRG)神经元的动作电位数量。通过硬膜途径给予Tat-CBD3A6K (30 µM/animal) 能够减少由萜类生物碱辣椒素引发的大鼠硬脑膜血流增加。
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。
T83739	Myr-Tat-CBD3 TFA Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3
	Myr-Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白-蛋白相互作用的抑制剂。在10 µM的浓度下，该化合物能够约81%地抑制Cav2.2-CRMP2相互作用，并在大鼠初级背根神经节(DRG)神经元中抑制钾诱导的钙流入（IC50约为2.8 µM）。在20 µM的浓度下，Myr-Tat-CBD3能抑制钙电流，但不影响钠电流，在初级DRG神经元中表现出这种特性。经过脊髓内给药，myr-Tat-CBD3（20 µg/5 µl）能够防止大鼠脚掌撤回潜伏期因carrageenan注射而减少。此外，Myr-Tat-CBD3减少大鼠因线索引起的寻求可卡因行为的复发。

化合物

Cat.No: T10466

Target: P2X Receptor

Cat.No: T9216

Synonym: MLT943

Target: MALT

Cat.No: T36534

Synonym: SDZ 224015

Target: IL Receptor, Caspase

Cat.No: T36619

Target: Prostaglandin Receptor

Cat.No: T68025

Target: Others

Cat.No: T70618

Cat.No: T24950

Synonym: VUF 10214,VUF10214

Cat.No: T27752

Synonym: KT-109,KT 109

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

Cat.No: T38109

Anti-inflammatory agent 40

Cat.No: T78967

Target: Parasite

8(S),15(S)-DiHETE

Cat.No: T37156

Cat.No: T38209

Cat.No: T38327

Anti-inflammatory agent 64

Cat.No: T83048

Target: ROS Kinase

Mambalgin 1 TFA

Cat.No: T75954

Cat.No: T68393

Cat.No: T36101

Cat.No: TP1408

Cat.No: T69451

N-Oleoyl Glutamine

Cat.No: T36064

Reduced Haloperidol

Cat.No: T37167

Cat.No: TP2003

Tat-AKAP79 (326-336) TFA

Cat.No: T83728

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

Cat.No: T37182

Cat.No: T64113

Cat.No: T83143

Cat.No: T71212

L-AP4 monohydrate

Cat.No: T37127

Synonym: L-AP4 monohydrate

Galanin (Human) (Acetate)

Cat.No: T38110

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Cat.No: T83875

Tat-CBD3A6K TFA

Cat.No: T83732

Cat.No: T83674

Myr-Tat-CBD3 TFA

Cat.No: T83739

Synonym: Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3

Cat. No.	Product Name	Target	Signaling Pathways
T7907	7-Methoxyflavone	Others	Others
	7-Methoxyflavone 是一种分离自 Zornia brasiliensis 的化合物。它能够抑制福尔马林疼痛反应神经源期的舔爪时间 (65.6%)，有外周镇痛活性，但不影响炎症期的伤害性反映。
T5781	taraxasteryl acetate 蒲公英甾醇醋酸酯,醋酸蒲公英酯	Antibacterial	Microbiology/Virology
	Taraxasteryl acetate 是分离自矢状疟原虫中，具有广谱的抗炎活性。它能够改善右旋糖酐、酵母聚糖及花生四烯酸诱导的大鼠后爪水肿。它可用于研究局部炎症。
T4S0176	Alnustone (4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one,桤木酮	Others	Others
	Alnustone ((4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one) 是一种非酚双苯庚烷类化合物，在草药和香料中发现，是姜黄的成分之一，具有抗吐、抗炎作用。
TN4493	Mannioside A
	Mannioside A has anti-inflammatory activity, inhibits carrageenan-induced paw edema in the rat.
TN1364	Ajugasterone C 筋骨草甾酮 C,筋骨草甾酮C
	Ajugasterone C shows significant inhibitory effect at 100 mg/kg dose on rat paw oedema development due to carrageenan-induced inflammation in Sprague Dawley rats.
TN4406	Lamiide
	Lamiide has anti-inflammatory activity in carrageenin-induced paw edema test. It shows lipid peroxidation inhibition on rat-brain phospholipid peroxidation.
TN5477	GB-2a
	GB 2a shows antioxidant and anti-inflammatory effects, it can prevent the carrageenan-induced paw oedema. GB 2a biflavonoid can promote inhibition on tyrosinase activity and reduced melanin biosynthesis in B16F10 cells, which suggests great potential for
TN1623	Escin IIB	Others; NOS	Immunology/Inflammation; Others
	Escin IIB has positive effects on acute inflammation in animals, it can inhibit the induced by serotonin in rats, the hind paw edema induced by carrageenin, and the scratching behavior induced by compound 48/80 in mice.
TN3447	Arjunglucoside I
	Arjunglucoside I has anti-inflammatory activity, it exhibits significant activity against carrageenan-induced paw edema in rat. It also shows antiproliferative activity against the A2780 human ovarian cancer cell line with an IC(50) value of 1.2 microM.
TN1606	(-)-Epiafzelechin (-)-表阿夫儿茶精,表阿夫儿茶精	COX	Immunology/Inflammation; Neuroscience
	(-)-Epiafzelechin exhibits significant anti-inflammatory activity on carrageenin-induced mouse paw edema, it exhibits a dose-dependent inhibition on the COX activity with an IC50 value of 15 microM, it exhibits about 3-fold weaker inhibitory potency on th
TN1080	Kaji-ichigoside F1 蔷薇苷
	Kaji-ichigoside F1 shows antiinflammatory/antinociceptive action in acetic acid-induced writhing and hot plate testing and in a carrageenan-induced paw edema model in mice and rats. Kaji-ichigoside F1 exhibits in vivo hepatoprotective effects, it inhibite
TN5466	Boeravinone B
	Boeravinone B, a novel efflux pump inhibitor, apart from inhibiting the MdeA mediated efflux, also significantly inhibit the biofilm formation of S. aureus, boeravinone B may be used in combination with mupirocin for further development. Boeravinone B exh
TN4505	Masticadienolic acid	Others	Others
	Masticadienolic acid is a specific competitive inhibitor of secreted phospholipase A2, it not only protects the active site histidine from alkylation but also inhibits the action of secreted from pancreas, synovial fluid, and bee venom. Masticadienolic ac

天然产物

7-Methoxyflavone

Cat.No: T7907

Target: Others

taraxasteryl acetate

Cat.No: T5781

Synonym: 蒲公英甾醇醋酸酯,醋酸蒲公英酯

Target: Antibacterial

Cat.No: T4S0176

Synonym: (4E,6E)-1,7-Diphenyl-4,6-heptadien-3-one,桤木酮

Target: Others

Cat.No: TN4493

Cat.No: TN1364

Synonym: 筋骨草甾酮 C,筋骨草甾酮C

Cat.No: TN4406

Cat.No: TN5477

Cat.No: TN1623

Target: Others, NOS

Arjunglucoside I

Cat.No: TN3447

(-)-Epiafzelechin

Cat.No: TN1606

Synonym: (-)-表阿夫儿茶精,表阿夫儿茶精

Target: COX

Kaji-ichigoside F1

Cat.No: TN1080

Synonym: 蔷薇苷

Cat.No: TN5466

Masticadienolic acid

Cat.No: TN4505

Target: Others

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