| Bioactivity | Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research[1][2]. | ||||||||||||
| Invitro | C1 inhibitor (C1INH) is the primary regulator of contact activation, both by inhibiting the conversion of prekallikrein to plasma kallikrein (PKK) by FXIIa, and by directly inhibiting PKK. PKK cleaves high molecular weight kininogen, releasing bradykinin, whose actions are responsible for the signs and symptoms of hereditary angioedema (HAE)[2]. | ||||||||||||
| Name | Avoralstat | ||||||||||||
| CAS | 918407-35-9 | ||||||||||||
| Formula | C28H27N5O5 | ||||||||||||
| Molar Mass | 513.54 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Aygoren-Pursun E, et al. Prophylaxis of hereditary angioedema attacks: A randomized trial of oral plasma kallikrein inhibition with avoralstat. J Allergy Clin Immunol. 2016 Sep;138(3):934-936.e5. [2]. Cornpropst M, et al. Safety, pharmacokinetics, and pharmacodynamics of avoralstat, an oral plasma kallikrein inhibitor: phase 1 study. Allergy. 2016;71(12):1676-1683. |
Avoralstat
CAS: 918407-35-9 F: C28H27N5O5 W: 513.54
Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema re
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