BMS-582949是一种口服活性强、高度选择性的p38α MAP激酶抑制剂,对p38α的IC50为13 nM,对TNFα为50 nM。可用于类风湿关节炎的研究。
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| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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| 产品名称 | p38 MAPK ↓ ↑ | p38α ↓ ↑ | p38β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| BMS-582949 |
+++
p38 MAPK, IC50: 13 nM |
98% | |||||||||||||||||
| Adezmapimod | 99%+ | ||||||||||||||||||
| Pexmetinib | ✔ | Tie-2 | 99%+ | ||||||||||||||||
| Skepinone-L |
++++
p38α, IC50: 5 nM |
98% | |||||||||||||||||
| Doramapimod |
++++
p38α, Kd: 0.1 nM p38α, IC50: 38 nM |
99%+ | |||||||||||||||||
| VX-702 | 99%+ | ||||||||||||||||||
| Ralimetinib dimesylate |
++++
p38α, IC50: 7 nM |
98% | |||||||||||||||||
| SB 202190 |
++
p38α, IC50: 50 nM |
++
p38β, IC50: 100 nM |
99%+ | ||||||||||||||||
| Losmapimod |
++++
p38α, pKi: 8.1 |
+++
p38β, pKi: 7.6 |
99%+ | ||||||||||||||||
| Neflamapimod |
+++
p38α, IC50: 10 nM |
+
p38β, IC50: 220 nM |
99%+ | ||||||||||||||||
| PH-797804 |
++
p38α, IC50: 26 nM |
+
p38β, IC50: 102 nM |
99% | ||||||||||||||||
| TAK-715 |
++++
p38α, IC50: 7.1 nM |
+
p38β, IC50: 0.20 μM |
99%+ | ||||||||||||||||
| SB 239063 |
++
p38α, IC50: 44 nM |
++
p38β, IC50: 44 nM |
99%+ | ||||||||||||||||
| Pamapimod |
+++
p38α, IC50: 0.014 μM |
+
p38β, IC50: 0.48 μM |
98%+ | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13 nM,inhibiting both p38 kinase activity and activation of p38. |
| Administration | Dosage | Frequency | Description | References | ||
| Rats | Subarachnoid hemorrhage model | Intraperitoneal injection | 100 mg/kg | Single administration | BMS-582949 significantly decreased the protein expression levels of p-p38, significantly downregulated the expression levels of oxidative stress and apoptosis-associated proteins, but had no significant effect on the protein expression levels of p-ASK1, ASK1, or p-JNK. | Mol Med Rep. 2023 Feb;27(2):47 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.46mL 0.49mL 0.25mL |
12.30mL 2.46mL 1.23mL |
24.60mL 4.92mL 2.46mL |
|
| CAS号 | 623152-17-0 |
| 分子式 | C22H26N6O2 |
| 分子量 | 406.48 |
| SMILES Code | O=C(C1=CN2N=CN=C(NC3=CC(C(NC4CC4)=O)=CC=C3C)C2=C1C)NCCC |
| MDL No. | N/A |
| 别名 | PS540446 |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
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