R116031
Catalog No. A62116

R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist, demonstrating a Ki value of 0.45 nM against the human NK-1 receptor. This compound effectively inhibits Substance P-induced peripheral responses, such as skin reactions and plasma extravasation in guinea pig models, as well as central effects demonstrated in gerbils. Additionally, R116031, when labeled with 3H, shows significant accumulation in brain regions including the striatum, olfactory tubercle, olfactory bulb, and locus coeruleus, making it suitable for use as a PET ligand in imaging studies.
Chemical Information
| Catalog Num | A62116 |
|---|---|
| M. Wt | 660.69 |
| Formula | C35H38F6N4O2 |
| Purity | >98% |
| Storage | at -20 °C 3 years (powder form); at -20 °C 6 months (Solution base) |
| CAS No. | 336884-84-5 |
| Synonyms | |
| SMILES | O=C(C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)N2[C@@H](C[C@@H](N3CCN(CC3)CC(NC4=C(C=CC=C4C)C)=O)CC2)CC5=CC=CC=C5 |
Biological Activity
| Description | R116031 is a selective Neurokinin-1 (NK-1) receptor antagonist, demonstrating a Ki value of 0.45 nM against the human NK-1 receptor. This compound effectively inhibits Substance P-induced peripheral responses, such as skin reactions and plasma extravasation in guinea pig models, as well as central effects demonstrated in gerbils. Additionally, R116031, when labeled with 3H, shows significant accumulation in brain regions including the striatum, olfactory tubercle, olfactory bulb, and locus coeruleus, making it suitable for use as a PET ligand in imaging studies. |
|---|
RETURN POLICY
Adooq’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
Adooq’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.


