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- 2025年07月23日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
BMS-378806
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
357263-13-9
- 规格：
50mg/25mg/10mg/1mg/5mg
| 规格： | 50mg | 产品价格： | ￥3428.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥2328.0 |
| 规格： | 10mg | 产品价格： | ￥1175.0 |
| 规格： | 1mg | 产品价格： | ￥286.0 |
| 规格： | 5mg | 产品价格： | ￥674.0 |
| 基本信息 | |
| CAS | No.357263-13-9 |
| 英文名称 | BMS-378806 |
| 别名 | BMS 806;1-[(2R)-4-苯甲酰基-2-甲基-1-哌嗪基]-2-(4-甲氧基-1H-C4H5N并[2;3-B]吡啶-3-基)-1;2-乙二酮 |
| 分子式 | C22H22N4O4 |
| 分子量 | 406.43 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | CC1CN(CCN1C(=O)C(=O)C2=CNC3=NC=CC(=C23)OC)C(=O)C4=CC=CC=C4 |
| InChIKey | OKGPFTLYBPQBIX-CQSZACIVSA-N |
| InChI | InChI=1S/C22H22N4O4/c1-14-13-25(21(28)15-6-4-3-5-7-15)10-11-26(14)22(29)19(27)16-12-24-20-18(16)17(30-2)8-9-23-20/h3-9，12，14H，10-11，13H2，1-2H3，(H，23，24)/t14-/m1/s1 |
| PubChem CID | 5495818 |
| 靶点 | HIV-1 |
| 通路 | Anti-infection |
| 背景说明 | BMS-378806 是一种有效的 HIV-1 抑制剂，干扰 CD4-gp120 相互作用。BMS-378806选择性抑制 HIV-1 gp120 结合到 CD4 受体。 |
| 生物活性 | BMS-378806 is a potent HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. BMS-378806 selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus.[1][2][3] |
| In Vitro | 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[1]. 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)[2]. 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 specific region within the CD4 binding pocket of gp120 by using HIV-1 gp120 variants carrying either compound-selected resistant substitutions or gp120-CD4 contact site mutations[3]. |
| 细胞实验 | 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[1]. |
| 动物实验 | Rats， Dogs and Monkeys[1]The pharmacokinetic properties of BMS-378806 in the rat， dog， and cynomolgus monkey are summarized. The oral bioavailability of BMS-378806 in rats， administered as a solution in PEG 400/EtOH (90:10 v/v)， is 19% at a dose of 5 mg/kg while an aqueous crystalline suspension of free base in 0.75% (w/w) Methocel A4M Premium administered orally at the same dose afforded a relative bioavailability of 61%. |
| 激酶实验 | To measure gp120-CD4 binding， the wild-type or variant gp120 proteins are first captured onto a plate by D7324 antibody. CD4 binding is initiated by adding sCD4 to a gp120-coated plate. To determine the ability of BMS-378806 to compete with sCD4 for gp120 binding， the compound is added simultaneously with sCD4 and reactions are carried out in buffer C (50 mM Tris-HCl [pH 7.5]， 100 mM NaCl， 1% bovine serum albumin) for 2 h at room temperature. After washing with buffer B (20 mM Tris-HCl， 500 mM NaCl， 0.05% Tween 20 [pH 7.5])， the bound CD4 is detected with OKT4 antibody (0.36 μg/mL) and goat anti-mouse peroxidase conjugate. Bound antibody is detected with 3，3′，5，5′-tetramethylbenzidine chromogenic substrate for peroxidase[3]. |
| 数据来源文献 | [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 |
| 单位 | 瓶 |
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￥286 - 3428
