H2521264计算溶液所需的质量、体积或浓度。
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
|---|
BMS-986278
有货
为什么选择此级别
Moligand™ 级 提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with K b s of 6.9 nM and 4.0 nM for human and mouse LPA1, respectively. BMS-986278 can be used for the research of pulmonary fibrotic diseases
In Vitro
BMS-986278 is a high-affinity LPA1 antagonist, with K b s of 6.9 nM and 4.0 nM for human and mouse LPA1 in CHO cells overexpressing LPA1. BMS-986278 antagonizes Lysophosphatidic acid (LPA)-stimulated calcium flux in normal human lung fibroblasts, with a K b of 5.8 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BMS-986278 (0.1-10 mg/kg; a single p.o.) completely inhibits LPA-stimulated systemic histamine release in a concentration-dependent manner in CD1 mice . BMS-986278 (3-30 mg/kg; p.o. twice daily for 14 d) decreases Bleomycin-induced collagen deposition/lung fibrosis in rats . Pharmacokinetics of BMS-986278 in preclinical species plasma clearance ((mL/min)/kg) V ss (L/kg) oral bioavailability (%) T 1/2 (h) plasma protein binding (% free) mouse 37 5.5 70 2.5 31.4 rat 15 3.5 100 4.5 12.6 monkey 2.0 1.6 79 11 0.8 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (10 weeks) were administered Bleomycin Dosage: 3, 10, and 30 mg/kg Administration: P.o. twice daily for 14 days Result: Resulted in significant decreases in the lung section percent fibrotic area for the 3 mg/kg (48%) and 10 mg/kg (56%) dose groups.
Form:Solid
IC50& Target:Kb: 6.9 nM (human LPA1), 4.0 nM (mouse LPA1)
规格
规格或纯度
Moligand™, ≥99%
英文名称
BMS-986278
生化机理
BMS-986278 是一种溶血磷脂酸受体 1（LPA1）拮抗剂，对人类和小鼠 LPA1 的 K b s 分别为 6.9 nM 和 4.0 nM。BMS-986278 可用于肺纤维化疾病的研究。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
拮抗剂
纯度
≥99%
名称和识别符
技术文档
高级数据
关联靶点（人）
KCNH2
Tclin
HERG
(29587 活性数据)
CYP2C8
Tchem
Cytochrome P450 2C8
(1492 活性数据)
LPAR1
Tchem
Lysophosphatidic acid receptor Edg-2
(779 活性数据)
CYP2D6
Tclin
Cytochrome P450 2D6
(33882 活性数据)
CYP1A2
Tchem
Cytochrome P450 1A2
(26471 活性数据)
CYP2C9
Tchem
Cytochrome P450 2C9
(32119 活性数据)
CYP2C19
Tchem
Cytochrome P450 2C19
(29246 活性数据)
CYP3A4
Tclin
Cytochrome P450 3A4
(53859 活性数据)
CYP2B6
Tchem
Cytochrome P450 2B6
(1338 活性数据)
ABCB11
Tchem
Bile salt export pump
(2311 活性数据)
ABCC3
Tbio
Canalicular multispecific organic anion transporter 2
(718 活性数据)
SLCO1B1
Tchem
Solute carrier organic anion transporter family member 1B1
(2672 活性数据)
SLCO1B3
Tchem
Solute carrier organic anion transporter family member 1B3
(2517 活性数据)
ABCC4
Tchem
Multidrug resistance-associated protein 4
(785 活性数据)
ABCB4
Tbio
Multidrug resistance protein 3
(8 活性数据)
关联靶点（其它种属）
Rattus norvegicus (775804 活性数据)
Lpar1
Lysophosphatidic acid receptor 1 (7 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 100 mg/mL (224.46 mM; Need ultrasonic)
分子量
445.500 g/mol
XLogP3
2.100
氢键供体数Hydrogen Bond Donor Count
1
氢键受体数Hydrogen Bond Acceptor Count
8
可旋转键计数Rotatable Bond Count
9
精确质量Exact Mass
445.233 Da
单同位素质量Monoisotopic Mass
445.233 Da
拓扑极表面积Topological Polar Surface Area
120.000 Ų
重原子数Heavy Atom Count
32
形式电荷Formal Charge
0
复杂度Complexity
638.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
2
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
1
质检证书（CoA,COO,BSE/TSE 和分析图谱)
溶液计算器
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