Clobenpropit dihydrobromide
Cat. No.:YN320110
CAS No. :145231-35-2
产品名称: | Clobenpropit dihydrobromide |
CAS No.: | 145231-35-2 |
Chemical Name: | N-[(4-chlorophenyl)methyl]-carbamimidothioic acid, 3-(1H-imidazol-5-yl)propyl ester, dihydrobromide |
Synonyms: | VUF-9153;VUF9153 |
分子量: | 470.65 |
分子式: | C₁₄H₁₉Br₂ClN₄S |
SMILES: | N=C(SCCCC1=CN=CN1)NCC2=CC=C(Cl)C=C2.[H]Br.[H]Br |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Clobenpropit dihydrobromide 是一种有效的组胺H3R拮抗剂/反向激动剂,对组胺 H3LR 的pEC50为 8.07。Clobenpropit dihydrobromide 对组胺H4受体起部分激动剂的作用,Ki为 13 nM。Clobenpropit dihydrobromide 还与 5-HT3 受体 (Ki为 7.4 nM) 和 α2A/α2C 肾上腺素受体 (Ki为 17.4/7.8 nM) 结合。Clobenpropit dihydrobromide 促进凋亡 (apop |
IC50和靶点: | [{name:"Human H3LR:9.44 (pKi)"},{name: "Rat H3LR:9.75 (pKi)"},{name: "H4 receptor:13 nM (Ki)"},{name: "H2 Receptor:5.6 (pKi)"}] |
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Solt, L.A., Kumar, N., Nuhant, P., et al.Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligandNature472(7344),491-494(2011)
Yokoyama, H., Onodera, K., Maeyama, K., et al.Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in miceEur. J. Pharmacol.260(1),23-28(1994)
Dai, H., Fu, Q., Shen, Y., et al.The histamine H3 receptor antagonist clobenpropit enhances GABA release to protect against NMDA-induced excitotoxicity through the cAMP/protein kinase A pathway in cultured cortical neuronsEur. J. PHarmacol.563(1-3),117-123(2007)