规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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靶点 |
CCR5 ( IC50 = 3.6 nM ); CCR2 ( IC50 = 6.2 nM )
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体外研究 (In Vitro) |
BMS-813160 与 CCR2、CCR5、CCR1、CCR4 和 CXCR2 结合,IC50 分别为 6.2 nM、3.6 nM、>25 μM、>40 μM 和>40 μM[2]。 BMS-813160 显示出对 CCR2 CTX、CCR2 CD11b、CCR5 CTX 和 CCR5 CD11b 的活性,IC50 分别为 0.8、4.8、1.1 和 5.7 nM[2]。
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体内研究 (In Vivo) |
BMS-813160(10-160 mg/kg;口服,每天两次,持续两天)可抑制小鼠硫代乙醇酸盐诱导的腹膜炎模型中炎症单核细胞和巨噬细胞的迁移,并显示出优异的口服生物利用度[2]。动物模型:人CCR2敲入C57BL/6雄性小鼠,注射巯基乙酸盐[2] 剂量:10、50和160 mg/kg 给药方式:口服灌胃; 10-160毫克/公斤,每天两次;两天结果:腹膜中炎症单核细胞和巨噬细胞浸润呈剂量依赖性减少。
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动物实验 |
Human-CCR2 knock-in C57BL/6 male mice with thioglycollate injection
10, 50 and 160 mg/kg Oral gavage; 10-160 mg/kg twice a day; for two days |
参考文献 |
分子式 |
C25H40N8O2
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分子量 |
484.637504577637
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精确质量 |
484.33
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元素分析 |
C, 61.96; H, 8.32; N, 23.12; O, 6.60
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CAS号 |
1286279-29-5
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外观&性状 |
Solid powder
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SMILES |
CC(=O)N[C@@H]1C[C@@H](CC[C@@H]1N2CC[C@@H](C2=O)NC3=NC=NC4=CC(=NN43)C(C)(C)C)NC(C)(C)C
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InChi Key |
CMVHFGNTABZQJU-HCXYKTFWSA-N
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InChi Code |
InChI=1S/C25H40N8O2/c1-15(34)28-18-12-16(30-25(5,6)7)8-9-19(18)32-11-10-17(22(32)35)29-23-27-14-26-21-13-20(24(2,3)4)31-33(21)23/h13-14,16-19,30H,8-12H2,1-7H3,(H,28,34)(H,26,27,29)/t16-,17+,18-,19+/m1/s1
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化学名 |
N-[(1R,2S,5R)-5-(tert-butylamino)-2-[(3S)-3-[(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-yl)amino]-2-oxopyrrolidin-1-yl]cyclohexyl]acetamide
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别名 |
BMS813160; BMS-813160; BMS 813160
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO: 25~97 mg/mL (51.6~200.1 mM)
Ethanol: ~97 mg/mL |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0634 mL | 10.3169 mL | 20.6339 mL | |
5 mM | 0.4127 mL | 2.0634 mL | 4.1268 mL | |
10 mM | 0.2063 mL | 1.0317 mL | 2.0634 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT03496662 | Active Recruiting |
Drug: BMS-813160 Drug: Nivolumab |
Pancreatic Ductal Adenocarcinoma |
Washington University School of Medicine |
August 31, 2018 | Phase 1 Phase 2 |
NCT04123379 | Active Recruiting |
Drug: BMS-813160 Drug: Nivolumab |
Non-small Cell Lung Cancer Hepatocellular Carcinoma |
Icahn School of Medicine at Mount Sinai |
March 5, 2020 | Phase 2 |
NCT03767582 | Recruiting | Drug: Nivolumab Drug: GVAX |
PDAC Pancreatic Ductal Adenocarcinoma |
BSidney Kimmel Comprehensive Cancer Center at Johns Hopkins |
December 12, 2019 | Phase 1 Phase 2 |
NCT01049165 | Completed | Drug: BMS-813160 Drug: [14C] BMS-813160 |
Accelerated Intimal Hyperplasia | Bristol-Myers Squibb | February 2010 | Phase 1 |
NCT03184870 | Completed | Drug: BMS-813160 Biological: Nivolumab |
Colorectal Cancer Pancreatic Cancer |
Bristol-Myers Squibb | August 8, 2017 | Phase 1 Phase 2 |