AL 8810 CAS: 246246-19-5
MF: C24H31O4F
MW: 402.50
An 11β-fluoro analog of PGF2α which acts as a potent antagonist at the FP receptor.

AL 8810 (CAS 246246-19-5)

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应用; AL 8810 is an 11β-fluoro analog of PGF2α which acts as a potent antagonist at the FP receptor
CAS号码: 246246-19-5
纯度: ≥98%
分子量: 402.50
分子式: C24H31O4F
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).

AL 8810 is an 11β-fluoro analog of PGF2α which acts as a potent and selective antagonist at the PGF2αR (FP receptor). AL 8810 has weak intrinsic agonist activity on FP receptor preparations in the 200-300 nM range, yet it fully antagonizes the activity of the potent FP receptor agonist fluprostenol at this concentration, with EC50 values of approximately 430 nM. AL 8810 fully antagonized the bimatoprost-induced calcium mobilization in Swiss 3T3 fibroblasts at 100 μM, indicating that bimatoprost acts as an FP agonist in this preparation. The Ki for the inhibition of several potent agonists at the cloned human ciliary body FP receptor is in the range of 1-2 μM.


参考文献

1 Griffen, B.W., Klimko, P., Crider, J.Y., et al. AL-8810: A novel prostaglandin F2α analog with selective antagonist effects at the prostaglandin F2α (FP) receptor. J Pharmacol Exp Ther 290 1278-1284 (1999). 2 Sharif, N.A., Williams, G.W., Kelly, C.R. Bimatoprost and its free acid are prostaglandin FP receptor agonists. Eur J Pharmacol 432 211-213 (2001). 3 Sharif, N.A., Kelly, C.R., Crider, J.Y. Agonist activity of Bimatoprost, Travoprost, Latanoprost, Unoprostone isopropyl ester and other prostaglandin analogs at the cloned human ciliary body FP prostaglandin receptor. J Ocul Pharmacol 18 313-324 (2002 Feb 27).

物理状态 :
Solid
溶解度 :
Soluble in DMSO (~25 mg/ml), ethanol (~25 mg/ml), DMF (~25 mg/ml), PBS (pH 7.2) (~0.05 mg/ml), and water (0.05 mg/ml at 25° C).
保存 :
Store at -20° C
熔点 :
232.63° C (Predicted)
沸点 :
~594.6° C at 760 mmHg (Predicted)
密度 :
~1.2 g/cm3 (Predicted)
折射率 :
n20D 1.58 (Predicted)
IC50 :
Fully antagonizes the activity of the potent FP receptor agonist fluprostenol: EC5050 = ~430 nM
pK值 :
pKa: 4.76 (Predicted)
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
MDL 号码 :
MFCD04039992
SMILES :
C1[[email protected]@H]([[email protected]@H]([[email protected]]([[email protected]]1F)/C=C/[[email protected]@H](C2CC3=CC=CC=C3C2)O)C/C=C\\CCCC(=O)O)O

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