[CAS NO. 1809010-50-1] Berotralstat
PRODUCTS SPECIFICATIONS [1809010-50-1]
DESCRIPTION [1809010-50-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 562.56 |
| Molecular Formula | C30H26F4N6O |
| SMILES | O=C(C1=CC(C(F)(F)F)=NN1C2=CC(CN)=CC=C2)NC3=CC([C@@H](C4=CC(C#N)=CC=C4)NCC5CC5)=CC=C3F |
Summary
Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE [1] [2] .
IC50 & Target
Plasma kallikrein [1]
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04933721 | BioCryst Pharmaceuticals |
Hereditary Angioedema|HAE
|
July 23, 2021 | Phase 3 |
| NCT05453968 | BioCryst Pharmaceuticals |
Hereditary Angioedema|Pediatric
|
October 2022 | Phase 3 |
| NCT04428632 | BioCryst Pharmaceuticals |
Hereditary Angioedema|HAE|Prophylaxis
|
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL ( 177.76 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7776 mL | 8.8879 mL | 17.7759 mL |
| 5 mM | 0.3555 mL | 1.7776 mL | 3.5552 mL |
| 10 mM | 0.1778 mL | 0.8888 mL | 1.7776 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 8.5 mg/mL (15.11 mM); Clear solution
References
- [1] Zuraw B, et al. Oral once-daily berotralstat for the prevention of hereditary angioedema attacks: A randomized, double-blind, placebo-controlled phase 3 trial [published online ahead of print, 2020 Oct 21]. J Allergy Clin Immunol. 2020;S0091-6749(20)31484
- [2] Manning ME, et al. Berotralstat (BCX7353) is a novel oral prophylactic treatment for hereditary angioedema: Review of phase II and III studies. Allergy Asthma Proc. 2021;42(4):274-282.