Free shipping on all orders over $ 500

GLPG1837

Cat. No. M9097
GLPG1837 Structure
Synonym:

ABBV-974; GLPG-1837

Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 205  USD205 In stock
25mg USD 380  USD380 In stock
50mg USD 720  USD720 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

GLPG1837 is a potent CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. GLPG1837 increases the conductivity of the G551D CFTR channel with obtained potency of 181 nM. GLPG1837 shows enhanced efficacy on CFTR mutants harboring Class III mutations compared to Ivacaftor, the first marketed potentiator. GLPG1837 was generally safe and well tolerated in healthy subjects up to the highest dose of 800 mg twice daily for 2 weeks.

Chemical Information
Molecular Weight 348.42
Formula C16H20N4O3S
CAS Number 1654725-02-6
Solubility (25°C) DMSO: ≥ 100 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] Van der Plas SE, et al. J Med Chem. Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.

[2] Yeh HI, et al. J Gen Physiol. A common mechanism for CFTR potentiators.

Related CFTR Products
GLPG-3221 

GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC50 of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis.

Posenacaftor sodium

Posenacaftor (PTI-801) sodium is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor sodium is used for the research of cystic fibrosis (CF).

Posenacaftor

Posenacaftor (PTI-801) is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF).

Galicaftor

Galicaftor (ABBV-2222; GLPG-2222) is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Galicaftor can be used for cystic fibrosis research.

CFTR corrector 4 

CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 4 can increase CFTR levels at the cell surface and have the potential for treatment of cystic fibrosis.

  Catalog
Abmole Inhibitor Catalog




Keywords: GLPG1837, ABBV-974; GLPG-1837 supplier, CFTR, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.