RepaglinideA KIR6 (KATP) channel blocker

Repaglinide (CAS 135062-02-1)

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Synonym: (S)-2-Ethoxy-4-[2-[[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzoic Acid
Application: A KIR6 (KATP) channel blocker
CAS Number: 135062-02-1
Purity: ≥99%
Molecular Weight: 452.59
Molecular Formula: C27H36N2O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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Repaglinide is a KIR6 (KATP) channel blocker that binds with high affinity for SUR1 when co-expressed with KIR6.2(Kd = 0.42 nM).


References

Wolffenbuttel, B.H.R., et al.: Eur. J. Clin. Pharmacol., 45, 113 (1993), Ampudia-Blasco, F.J., et al.: Diabetologia, 37, 703 (1994),

Appearance :
Crystalline
Physical State :
Solid
Solubility :
Soluble in water (<1 mg/ml at 25° C), chloroform, methanol, DMSO (91 mg/ml at 25° C), and ethanol (91 mg/ml at 25° C).
Storage :
Store at -20° C
Melting Point :
126.1-127.8° C
Boiling Point :
~672.9° C at 760 mmHg (Predicted)
Density :
~1.1 g/cm3 (Predicted)
Refractive Index :
n20D 1.57 (Predicted)
Optical Activity :
α20/D +7.73º, c = 1.06 in methanol
IC50 :
whole- cell Kir6.2/SUR1 currents: IC50 = 21 nM; SUR1: IC50 = 106 nM (human); OCT1: IC50 = 9.2 µM (human)
pK Values :
pKa: 4.19 (Predicted), pKb: 5.78 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
RTECS :
DI0876305
PubChem CID :
65981
Merck Index :
14: 8136
MDL Number :
MFCD00906179
SMILES :
CCOC1=C(C=CC(CC(=O)N[C@@H](CC(C)C)C2=C(C=CC=C2)N2CCCCC2)=C1)C(O)=O

Download SDS (MSDS)

Certificate of Analysis

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Repaglinide  Product Citations

See how others have used Repaglinide. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 29996058  Chothe, PP.|Wu, SP.|Ye, Z.|Hariparsad, N.| et al. 2018. Mol. Pharm. 15: 4677-4688.

Citations 1 to 1 of 1 total
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