Structure
(L-2-Aminooxy-3-phenylpropanoic acid, CAS 42990-62-5)
BMS-986251 biochemical
BMS-986251
Purity
98%
Synonyms
BMS-986251; N/A; BMS-986251 biochemical
Purity/Purification
98%
CAS
2460133-35-9
Targets&IC50
RORbeta:10 uM (EC50), RORgammat:12 nM (EC50), IL-17:24 nM (EC50), RORalpha:10 uM (EC50)
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
In vitro
BMS-986251 (5-45 mg/kg; orally; twice daily until day 9) results in reduced ear thickness[1]. BMS-986251 (0.13, 0.79, 4.76 mg/kg; orally; once a day) displays a dose-dependent reduction of the IL-17F produced in naive C57BL/6 female mice (7-9 weeks)[1]. BMS-986251 (2 mg/kg of IV and 4 mg/kg of PO) has a T 1/2 of 7.7 hours, a CL of 2.7 mL/min/kg, and a V ss of 1.9 L/kg for IV in mouse[1]. Animal Model: C57BL/6 female mice with acanthosis[1]. Dosage: 5, 15, 45 mg/kg. Administration: Orally; twice daily until day 9. Result: Resulted in reduced ear thickness and significantly reduces imiquimod (IMQ)-induced skin thickening. Animal Model: Mouse or rat[1]. Dosage: 2 mg/kg of IV and 4 mg/kg of PO (Pharmacokinetic Analysis). Administration: IV or PO. Result: Had a T 1/2 of 7.7 hours, a CL of 2.7 mL/min/kg, and a V ss of 1.9 L/kg for IV in mouse. Had a C max of 4.8 uM and an AUC of 37 uM/h for PO in mouse. Had a T 1/2 of 11 hours, a CL of 1.3 mL/min/kg, and a V ss of 1.25 L/kg for IV in rat. Had a C max of 4.7 uM and an AUC of 64 uM/h for PO in rat.
Preparation and Storage
Powder: -20 degree C for 3 years
In solvent: -80 degree C for 2 years
In solvent: -80 degree C for 2 years
Structure
(L-2-Aminooxy-3-phenylpropanoic acid, CAS 42990-62-5)
Structure
(L-2-Aminooxy-3-phenylpropanoic acid, CAS 42990-62-5)
Structure
(L-2-Aminooxy-3-phenylpropanoic acid, CAS 42990-62-5)
Structure
(L-2-Aminooxy-3-phenylpropanoic acid, CAS 42990-62-5)
Related Product Information for BMS-986251 biochemical
BMS-986251 is an orally active and selective RORgammat inverse agonist with an EC 50 of 12 nM for RORgammat GAL4. BMS-986251 inhibits IL-17 with an EC 50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
References
1. NikolausAmrhein, et al. alpha-aminooxy-beta-phenylpropionic acid — a potent inhibitor of L-phenylalanine ammonia-lyase in vitro and in vivo. Plant Science Letters Volume 8, Issue 4, April 1977, Pages 313-317.
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Product Notes
The BMS-986251 (Catalog #AAA228457) is a Biochemical and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "BMS-986251, Biochemical" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
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Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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