MDR-652

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MDR-652 是非刺激性瞬时受体电位香草酸 1 (TRPV1) 的高度特异性和有效的激动剂，hTRPV1 和 rTRPV1 的 Ki 值分别为 11.4 nM 和 23.8 nM，hTRPV1 和 rTRPV1 的 EC50 分别为 5.05 和 93 nM。

MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1) with Ki value of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1 respectively and EC50s for hTRPV1 and rTRPV1 are 5.05 and 93 nM respectively. MDR-652 is a potent topical analgesic.(In Vivo):MDR-652 (0.5 and 5 mg/kg) displays a dose-dependent decrease of body temperature, supporting that MDR-652 displays TRPV1 agonism in the intact animal. Potent analgesic activity was observed in models of neuropathic pain, and MDR-652 blocked capsaicin induced allodynia, showing dermal accumulation with little transdermal absorption. MDR-652 (5-10 mg/kg; i.p. and s.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) . MDR-652 has a promising topical pharmacokinetic profile. MDR-652 displays weak systemic toxicity and is negative in assays of genotoxicity. In a single-dose toxicity study, the LD50 of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively.

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MDR-652 (0.5 and 5 mg/kg) displays a dose-dependent decrease of body temperature, supporting that MDR-652 displays TRPV1 agonism in the intact animal.MDR-652 (5-10 mg/kg; i.p. ands.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) . MDR-652 has a promising topical pharmacokinetic profile. MDR-652 has no significant toxicity. In a single-dose toxicity study, the LD50 of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively. Animal Model:ICR mouse Dosage:0.5 and 5 mg/kg Administration:Administered intraperitoneally; 7 hours Result:Decreased body temperature in a dose-dependent manner.Animal Model:Rats with spinal nerve ligation (SNL) model Dosage:1, 2, 5, and 10 mg/kg Administration:Administered intraperitoneally and subcutaneously; 24 hours Result:The i.p. administration exhibited an excellent and dose dependent analgesic profile with an ED50 of 0.5-2 mg/kg.The subcutaneous injection (sc) also displayed an excellent analgesic outcome with maximum effect at 30 min after administration.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

BET bromodomain|Apoptosis|BRD2|BRD3|BRD4

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1933528-96-1

447.95

C22H23ClFN3O2S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (558.10 mM)

CC(C)(C)c1nc(-c2cccc(Cl)c2)c(CNC(Nc2cc(F)c(CO)cc2)=O)s1

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(-20℃)

With Ice Pack

≥ 2 years