TargetMol

ICA-105665

Product Code:
 
TAR-T11606
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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CodeSizePrice
TAR-T11606-100mg100mg£1,066.00
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TAR-T11606-200mg200mg£1,579.00
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Further Information

Bioactivity:
ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 had low cytotoxic potential in human hepatocytes but inhibited liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 uM). ICA-105665 can penetrate the central nervous system (CNS) and has antiseizure effects[1][2][3][4].
CAS:
2694728-63-5
Formula:
C19H15F2N3O2
Molecular Weight:
355.3381
Purity:
0.98
SMILES:
Fc1ccc(CC(=O)Nn2c(nc3cc(F)ccc3c2=O)C2CC2)cc1

References

Generaux G, et al. Quantitative systems toxicology (QST) reproduces species differences in PF-04895162 liver safety due to combined mitochondrial and bile acid toxicity. Pharmacol Res Perspect. 2019 Oct 9;7(6):e00523. Aleo MD, et al. Phase I study of PF?04895162, a Kv7 channel opener, reveals unexpected hepatotoxicity in healthy subjects, but not rats or monkeys: clinical evidence of disrupted bile acid homeostasis. Pharmacol Res Perspect. 2019 Feb;7(1):e00467. Kasteleijn-Nolst Trenit? DG, et al. Kv7 potassium channel activation with ICA-105665 reduces photoparoxysmal EEG responses in patients with epilepsy. Epilepsia. 2013 Aug;54(8):1437-43. Bialer M, et al. Progress report on new antiepileptic drugs: a summary of the Eleventh Eilat Conference (EILAT XI). Epilepsy Res. 2013 Jan;103(1):2-30.