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AM095 是一种有效的 LPA1 受体拮抗剂,对重组人或小鼠 LPA1 的 IC50 值分别为 0.98 和 0.73 μM。
AM095 是一种有效的 LPA1 受体拮抗剂,对重组人或小鼠 LPA1 的 IC50 值分别为 0.98 和 0.73 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 496 | 现货 | |
2 mg | ¥ 736 | 现货 | |
5 mg | ¥ 1,180 | 现货 | |
10 mg | ¥ 1,860 | 现货 | |
25 mg | ¥ 3,150 | 现货 | |
50 mg | ¥ 4,620 | 现货 | |
100 mg | ¥ 6,590 | 现货 |
产品描述 | AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively. |
靶点活性 | LPA1 (mouse):0.73 μM, LPA1 (recombinant human):0.98 μM |
体外活性 | AM095是一种强效的LPA1受体拮抗剂,其通过抑制GTPγS与大量表达重组人类或鼠类LPA1的中国仓鼠卵巢(CHO)细胞膜的结合来发挥作用,其IC50值分别为0.98和0.73 μM。此外,AM095能够抑制大量表达鼠LPA1的CHO细胞(IC50=778 nM)和人类A2058黑色素瘤细胞(IC50=233 nM)中由LPA驱动的趋化作用。AM095在人类LPA1 GTPγS结合测定中的IC50与我们之前发表的化合物AM966(IC50=0.98±0.17 μM)和Debio-0719化合物(IC50=0.60±0.04 μM)相当[1]。AM095还能抑制稳定转染有人类或鼠类LPA1的CHO细胞中由LPA引起的钙通量,其对于LPA引起的人类或鼠类LPA1-转染CHO细胞钙通量的拮抗作用IC50值分别为0.025和0.023 μM[2]。 |
体内活性 | AM095具有高口服生物利用度和中等半衰期,在大鼠和犬类中口服和静脉注射给药时耐受性良好。在大鼠口服给药(10 mg/kg)后,AM095的血浆浓度在2小时达到峰值,Cmax为41 μM,之后在24小时降至10 nM。静脉注射(2 mg/kg)后,15分钟内观察到Cmax为12 μM,24小时后也降至约10 nM,半衰期为1.79小时。在犬类中,单次口服给药5 mg/kg,15分钟内血浆浓度达到峰值21 μM,24小时后降至10 nM。相比之下,静脉注射给药2 mg/kg,15分钟内达到Cmax 11 μM,并在8小时降至15 nM,半衰期为1.5小时[1]。 |
激酶实验 | Known amounts of AM095 (diluted in DMSO) or vehicle (DMSO) are added to 25 to 40 μg of hLPA1/CHO or mLPA1/CHO membranes and 0.1 nM [35S]-GTPγS in buffer (50 mM HEPES, 0.1 mM NaCl, 10 mM MgCl2, 50 μg/mL saponin, pH 7.5) containing 0.2% fatty acid-free human serum albumin and 5 μM GDP. To test for LPA1 antagonist activity, the ability of AM095 to inhibit GTPγS binding stimulated by 900 nM LPA (18:1) is measured. Alternatively, to test for agonist effects, the ability of AM095 to stimulate GTPγS binding in the absence of LPA is measured. Reactions are incubated for 30 min at 30°C, before harvesting membranes onto glass filter binding plates (UniFilter GF/B) and washing three times with cold buffer containing 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM MgCl2 using a Brandel 96-tip cell harvester. Plates are dried and then cpm are evaluated by using a Packard TopCount NXT microplate scintillation counter[1]. |
分子量 | 478.47 |
分子式 | C27H23N2NaO5 |
CAS No. | 1345614-59-6 |
Smiles | [Na+].C[C@@H](OC(=O)Nc1c(C)noc1-c1ccc(cc1)-c1ccc(CC([O-])=O)cc1)c1ccccc1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 5.5 mg/mL (11.49 mM), Sonication is recommended. | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
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