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Technical Data
| Formula | C16H20N4O3S |
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| Molecular Weight | 348.42 | CAS No. | 1654725-02-6 | |
| Solubility (25°C)* | In vitro | DMSO | 69 mg/mL (198.03 mM) | |
| Ethanol | 5 mg/mL (14.35 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | GLPG1837 (ABBV-974) is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor. | ||||
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| Targets |
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| In vitro | GLPG1837 has an attractive in vitro ADME profile, showing low Clint,unb in both microsomal and hepatocytes stability assays, good permeability, and no off-target inhibition of CYPs and the hERG channel[1]. | ||||
| In vivo | The pharmacokinetic profile of GLPG1837 is attractive, showing a low Cl,unb and good F% in both rat and dog. The CL (L/h/kg) of GLPG1837 after intravenous injection of 1 mg/kg dose are 1.92 and 0.32 in rats and dogs, respectively. T1/2 is 1.84 h in rats while 3 h in dogs. After 5 mg/kg p.o, the oral availability of GLPG1837 in rat is 67%. In dogs, F%>100[1]. |
Protocol (from reference)
Selleck's GLPG1837 has been cited by 7 publications
| Molecular dynamics and functional characterization of I37R-CFTR lasso mutation provide insights into channel gating activity [ iScience, 2022, 25(1):103710] | PubMed: 35072004 |
| In Vitro Rescue of the Bile Acid Transport Function of ABCB11 Variants by CFTR Potentiators [ Int J Mol Sci, 2022, 23(18)10758] | PubMed: 36142670 |
| Pharmacological Responses of the G542X-CFTR to CFTR Modulators [ Front Mol Biosci, 2022, 9:921680] | PubMed: 35813815 |
| Primary human nasal epithelial cells: biobanking in the context of precision medicine [ Biology, 2022, (182)-] | PubMed: None |
| Primary Human Nasal Epithelial Cells: Biobanking in the Context of Precision Medicine [ J Vis Exp, 2022, (182)] | PubMed: 35532277 |
| Utilisation of CFTR orthologues to evaluate new therapies for cystic fibrosis [ University of Bristol, 2022, ] | PubMed: None |
| Nanomolar-potency 'co-potentiator' therapy for cystic fibrosis caused by a defined subset of minimal function CFTR mutants. [ Sci Rep, 2019, 9(1):17640] | PubMed: 31776420 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.