品牌	貨號	產品規格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S81464-5mg	98%	￥765.00元	6	-	-	-
源葉(MedMol)	S81464-10mg	98%	￥1020.00元	7	-	-	-
源葉(MedMol)	S81464-25mg	98%	￥2040.00元	6	-	-	-
源葉(MedMol)	S81464-100mg	98%	￥6120.00元	預計交期：2-3天	-	-	-

產品介紹

BMS-378806 是一種有效的 HIV-1 抑制劑，干擾 CD4-gp120 相互作用。BMS-378806選擇性抑制 HIV-1 gp120 結合到 CD4 受體，EC50 為 0.85-26.5 nM。

產品描述：

BMS-378806 是一種有效的 HIV-1 抑制劑，干擾 CD4-gp120 相互作用。BMS-378806選擇性抑制 HIV-1 gp120 結合到 CD4 受體，EC50 為 0.85-26.5 nM。

靶點： HIV-1;HIV-2;gp120/CD4;?HIVProtease

體外研究：
In a series of biochemical assays, BMS-378806 is not an effective inhibitor of HIV integrase, protease, or reverse transcriptase, but did compete with soluble CD4 binding to a monomeric form of gp120 in an ELISA assay with IC50=100 nM. The specificity of BMS-378806 toward inhibition of HIV-1 is confirmed by evaluation against HIV-2, SIV, MuLV, RSV, HCMV, BVDV, VSV, and influenza virus, with no significant inhibitory activity observed at concentrations ranging from 10 to 30 μM and no overt cytotoxicity toward the host cells, CC50>225 μM. BMS-378806 is not a potent inhibitor of any of the five major human CYP isoforms, evaluated as recombinant preparations, with IC50 values of >100 μM for CYP1A2 and CYP2C9, 23 μM for CYP2C19, 20 μM for CYP2D6, and 39 to 81 μM for CYP3A4. Moreover, since BMS-378806 is metabolized by CYP450 1A2, 2D6, and 3A4, it is unlikely to lead to severe drug?drug interactions in a clinical setting. BMS-378806 inhibits viral replication by interfering with the binding interactions of gp120 with the cellular CD4 receptor. The IC50s determined for the gp120s from HIV LAI, BAL, NA420LN40, SF162, NL4-3, NA420B33, YU2, AD8, JRCSF, and 92US15.6 are 0.1, 0.1, 0.3, 0.5, 0.6, 0.7, 0.9, 1.0, 1.1, and 1.6 μM, respectively. A similar observation is also made for BMS-378806 (IC50s range from 0.2 to 9.6 μM). BMS-378806 binds directly to gp120 at a stoichiometry of approximately 1:1, with a binding affinity similar to that of soluble CD4. The potential BMS-378806 target site is localized to a spec

體內研究：
In toxicology studies, BMS-378806 is well tolerated in rats at doses of 100 mg/kg/day for 2 weeks and in dogs at doses of 90 mg/kg for 10 days. The dose-proportional increases in the AUC and Cmax are observed between doses of 5 and 25 mpk, when BMS-378806 is administered either in the solution or suspension formulation. In all three species, plasma levels of drug exceeded the concentrations required to half-maximally inhibit virus replication in vitro. The volume of distribution of BMS-378806 ranges from 0.4 to 0.6 L/kg, indicative of partitioning beyond plasma; however, examination of brain levels in the rat reveals minimal CNS penetration.

參考文獻：
1. Wang T, et al. Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. J Med Chem. 2003 Sep 25;46(20):4236-9.

2. Ho HT, et al. Envelope conformational changes induced by human immunodeficiency virus type 1 attachment inhibitors prevent CD4 binding and downstream entry events. J Virol. 2006 Apr;80(8):4017-25.

3. Guo Q, et al. Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactions. J Virol. 2003 Oct;77(19):10528-36

溶解性： Soluble in DMSO

保存條件： -20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.46 ml	12.302 ml	24.604 ml
5 mM	0.492 ml	2.46 ml	4.921 ml
10 mM	0.246 ml	1.23 ml	2.46 ml
50 mM	0.049 ml	0.246 ml	0.492 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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