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HJC0197

Cat. No. M11263
HJC0197  Structure
Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 155  USD155 In stock
50mg USD 435  USD435 In stock
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Quality Control & Documentation
Biological Activity

HJC0197 is a potent antagonist of Epac1 (the exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2). HJC0197 selectively blocked camp-induced Epac activation. HJC0197 inhibited epAC1-mediated RAP1-GDP exchange activity in the presence of isoconcentration of cAMP.

Chemical Information
Molecular Weight 339.45
Formula C19H21N3OS
CAS Number 1383539-73-8
Solubility (25°C) DMSO ≥ 40 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ryan B Griggs, et al. Neurobiol Dis. Methylglyoxal and a spinal TRPA1-AC1-Epac cascade facilitate pain in the db/db mouse model of type 2 diabetes

[2] Irene Ramos-Alvarez, et al. Am J Physiol Gastrointest Liver Physiol. Cyclic AMP-dependent protein kinase A and EPAC mediate VIP and secretin stimulation of PAK4 and activation of Na +,K +-ATPase in pancreatic acinar cells

[3] Chang-Hung Kuo, et al. Pulm Pharmacol Ther. Long-acting β2-adrenoreceptor agonists suppress type 1 interferon expression in human plasmacytoid dendritic cells via epigenetic regulation

[4] Tams Juhsz, et al. Cell Signal. Mechanical loading stimulates chondrogenesis via the PKA/CREB-Sox9 and PP2A pathways in chicken micromass cultures

[5] Holger Rehmann. Sci Rep. Epac-inhibitors: facts and artefacts

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