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Cat. No.: HY-174986

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CGRP antagonist 7

CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a K_i of 0.029 nM. CGRP antagonist 7 Inhibit the production of cyclic adenosine monophosphate (cAMP) with an IC₅₀ of 1.5 nM. CGRP antagonist 7 can be used for the study of migraine.

For research use only. We do not sell to patients.

CAS No.: 2173508-07-9
Formula: C₃₀H₃₂FN₅O₃
Molecular Weight:529.61

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

CGRP antagonist 7 Chemical Structure

CAS No.: 2173508-07-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

In Vitro

CGRP antagonist 7 (Compound 15) (0.1-10 μM, 0-60 min) exhibits the IC₅₀ more than 100 μM in human hepatocellular carcinoma (HepaRG) cells and moderate inhibition of CYP3A (IC₅₀ = 6.6 μM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Parmacokinetics

Species	Dose	Route	AUC_inf	T_1/2	CL_total	V_ss	C_max	T_max	F
Rat^[1].	1 mg/kg	i.v.	36709 min·ng/mL	40 min	28 mL/min/kg	777 mL/kg	/	/	/
Rat^[1].	10 mg/kg	p.o.	408768 min·ng/mL	/	/	/	2906 ng/mL	30 min	111 %

In Vivo

CGRP antagonist 7 (Compound 15) (1 mg/kg, i,p., single dose) significantly inhibits the increase in blood flow induced by CGRP in marmoset facial blood flow mode^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Marmoset facial blood flow mode induced by intravenous administration of hαCGRP at a dose of 10 μg/kg administered at −15, 15, 45, and 90 min^[1]
Dosage:

1 mg/kg
Administration:

Intraperitoneal injection (i.p.), single dose
Result:

Significantly inhibited the increase in facial blood flow induced by CGRP (E_max = 84% at 45 min).

Chemical Information

CAS No. 2173508-07-9
Molecular Weight 529.61
Formula C₃₀H₃₂FN₅O₃
SMILES

CC1=NNC(C(CC2=CC=C(C=C2C)C(NCC(N3[C@@H](CC[C@@H]3C(C)(C#N)C)C4=CC(F)=CC=C4)=O)=O)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Morita N, et al. Fragment-Based Discovery of an Oral Calcitonin Gene-Related Peptide Receptor Antagonist for the Treatment of Migraine. J Med Chem. 2025 Jul 24;68(14):14919-14944. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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