Product Name :
CP671305
Description:
CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.
CAS:
445295-04-5
Molecular Weight:
454.40
Formula:
C23H19FN2O7
Chemical Name:
(2R)-2-[4-([2-(2H-1,3-benzodioxol-5-yloxy)pyridin-3-yl]formamidomethyl)-3-fluorophenoxy]propanoic acid
Smiles :
C[C@@H](OC1=CC=C(CNC(=O)C2=CC=CN=C2OC2C=C3OCOC3=CC=2)C(F)=C1)C(O)=O
InChiKey:
CNIGFESSDPOCKS-CYBMUJFWSA-N
InChi :
InChI=1S/C23H19FN2O7/c1-13(23(28)29)32-15-5-4-14(18(24)9-15)11-26-21(27)17-3-2-8-25-22(17)33-16-6-7-19-20(10-16)31-12-30-19/h2-10,13H,11-12H2,1H3,(H,26,27)(H,28,29)/t13-/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
CP671305 is a potent, orally active, selective inhibitor of phosphodiesterase-4-D, and possesses high activities.|Product information|CAS Number: 445295-04-5|Molecular Weight: 454.40|Formula: C23H19FN2O7|Chemical Name: (2R)-2-[4-([2-(2H-1,3-benzodioxol-5-yloxy)pyridin-3-yl]formamidomethyl)-3-fluorophenoxy]propanoic acid|Smiles: C[C@@H](OC1=CC=C(CNC(=O)C2=CC=CN=C2OC2C=C3OCOC3=CC=2)C(F)=C1)C(O)=O|InChiKey: CNIGFESSDPOCKS-CYBMUJFWSA-N|InChi: InChI=1S/C23H19FN2O7/c1-13(23(28)29)32-15-5-4-14(18(24)9-15)11-26-21(27)17-3-2-8-25-22(17)33-16-6-7-19-20(10-16)31-12-30-19/h2-10,13H,11-12H2,1H3,(H,26,27)(H,28,29)/t13-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 100 mg/mL (220.07 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|CP-671,305 is identified as a substrate of MRP2 and BCRP, but not MDR1.FMK-MEA manufacturer CP-671,305 is a substrate of human OATP2B1 with a high affinity (Km=4 μM) but not a substrate for human OATP1B1 or OATP1B3.Mebendazole Protocol CP-671,305 displays high affinity (Km=12 μM) for rat hepatic Oatp1a4.PMID:32207840 CP-671,305 does not exhibit competitive inhibition of the five major cytochrome P450 enzymes, namely CYP1A2, 2C9, 2C19, 2D6 and 3A4 (IC50s > 50 μM). Likewise, no time-dependent inactivation of the five major cytochrome P450 enzymes is discernible with CP-671,305.|In Vivo:|CP-671,305 pharmacokinetics are largely unaltered, and compromised biliary clearance of CP-671,305 is compensated by increased urinary clearance. CP-671,305 demonstrates generally favourable pharmacokinetic properties, systemic plasma clearance after intravenous administration is low in Sprague-Dawley rats (9.60 ± 1.16 mL/min/kg), beagle dogs (2.90 ± 0.81 mL/min/kg) and cynomolgus monkeys (2.94 ± 0.87 mL/min/kg) resulting in plasma half-lives > 5 h. Moderate to high bioavailability in rats (43-80%), dogs (45%) and monkeys (26%) is observed after oral dosing. In rats, oral pharmacokinetics are dose dependent over the dose range studied (10 and 25 mg/kg).|Products are for research use only. Not for human use.|
