Vazegepant free base · Synonyms: BHV-3500 | Zavegepant
Vazegepant is the first intranasal CGRP receptor antagonist.
For research use only. Not for human or veterinary use.
Vazegepant structure
CAS No.: 1337918-83-8
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 100 mg | USD 420.00 | BP-01869-100mg | In stock | Get quote |
| 250 mg | USD 720.00 | BP-01869-250mg | In stock | Get quote |
| 500 mg | USD 1,120.00 | BP-01869-500mg | In stock | Get quote |
| 1 g | USD 1,720.00 | BP-01869-1g | In stock | Get quote |
| 5 g | Inquire | BP-01869-5g | Inquire | Inquire |
Need another size or custom synthesis? Request a quote.
Description
Vazegepant is the first intranasal CGRP receptor antagonist for the study the acute research of migraine.
Biological activity
In Vitro Vazegepant (Zavegepant) exhibits fully competitive binding activity to the human CGRP receptor expressed endogenously in the SKN-MC cell membrane, with a Ki of 23 pM, which is more than 10,000 times more selective than the adrenal medullary receptor 1/2, calcitonin receptor, and amyloid receptor 1/3; and can strongly and completely reverse the vasodilatory effect induced by CGRP in isolated human intracranial arterial tissue, with an EC50 of 880 pM. In Vivo Vazegepant (Zavegepant) (0.03 mg/kg; subcutaneous administration; 15-105 min) significantly inhibited CGRP-induced facial blood flow elevation in a marmoset model. Vazegepant exhibited low oral bioavailability in monkey (F = 0.3%), mouse (F = 1.4%), and rat (F = 1.7%) animal models. Vazegepant (nasal administration) was rapidly absorbed in a rabbit model, with a Tmax of 15-20 min.
Identifiers
- SMILES
-
O=C(N1CCC(C2=CC3=C(NC2=O)C=CC=C3)CC1)N[C@H](CC4=CC5=C(NN=C5)C(C)=C4)C(N6CCN(C7CCN(C)CC7)CC6)=O - InChIKey
-
JJVAPHYEOZSKJZ-JGCGQSQUSA-N
Specifications
- MW (average)
- 638.8022
- Formula
- C36H46N8O3
- CAS No.
- 1337918-83-8
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder 4°C, protect from light; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO 50 mg/mL