126050-12-2
126050-12-2 structure
- Name: neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)-
- Chemical Name: [TYR5,D-TRP6,8,9, ARG10]-NEUROKININ A(4-10)
- CAS Number: 126050-12-2
- Molecular Formula: C57H68N14O10
- Molecular Weight: 1109.238
- Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
- Create Date: 2018-06-28 01:34:41
- Modify Date: 2024-01-06 19:45:47
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MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively[1][2].
| Name | [TYR5,D-TRP6,8,9, ARG10]-NEUROKININ A(4-10) |
|---|---|
| Synonyms |
neurokinin A (4-10), Tyr(5)-Trp(6,8,9)-Arg(10)-
5-Tyr-6,8,9-Trp-10-Arg-NKA (4-10) 5-Tyr-6,8,9-Trp-10-Arg-neurokinin A (4-10) |
| Description | MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively[1][2]. |
|---|---|
| Related Catalog | |
| Target |
Tachykinin NK2 Receptor:7.9 (pA2) NK1:5.2 (pA2) NK3:4.9 (pA2) |
| In Vitro | In competitive radioligand binding assays, MEN 10207 (the IC50 ranges of 21-54 nM) has high affinity in bovine stomach membranes and SKLKB82#3 cells, a murine fibroblast cell line transfected with a cDNA encoding for the bovine NK2 receptor[3]. |
| In Vivo | but not Substance P in a dose-dependent manner. And MEN 10207 also effectively blocks the long-term reflex facilitation to the gastrocnemius nerve stimulation[1]. Animal Model: Decerebrate, spinalized, unanesthetized Female Sprague-Dawley rats (250-280 g)[1] Dosage: 7 pmol/10 μL, 70 pmol/10 μL, 700 pmol/10 μL Administration: Intrathecal administration; once Result: Blocked the reflex facilitation to intrathecal Neurokinin A, but not Substance P in a dose-dependent manner. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Molecular Formula | C57H68N14O10 |
| Molecular Weight | 1109.238 |
| Exact Mass | 1108.524292 |
| LogP | 3.11 |
| Index of Refraction | 1.711 |