(S)-AMG-628
(S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628 (HY-123374). (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin (HY-10448)- and acid-induced Ca2+-influx with IC50 of 7 nM and 5 nM in CHO cell. (S)-AMG-628 ameliorates Capsaicin-induced rats flinching, and reverses the thermal hypersensitivity in CFA-(HY-153808) induced inflammatory pain models.
For research use only. We do not sell to patients.
- CAS No.: 862269-92-9
- Formula: C25H25FN6O2S
- Molecular Weight:492.57
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
5 nM
Compound: 16q
|
Inhibition of rat TRPV1 expressed in CHO cells assessed as acid-induced Ca2+ influx
Inhibition of rat TRPV1 expressed in CHO cells assessed as acid-induced Ca2+ influx
|
[PMID: 17585751] |
| CHO | IC50 |
7 nM
Compound: 16q
|
Inhibition of rat TRPV1 expressed in CHO cells assessed as capsaicin-induced Ca2+ influx
Inhibition of rat TRPV1 expressed in CHO cells assessed as capsaicin-induced Ca2+ influx
|
[PMID: 17585751] |
Chemical Information
-
CAS No. 862269-92-9
-
Molecular Weight 492.57
-
Formula C25H25FN6O2S
-
SMILES
CC(NC1=NC(C(S1)=CC=C2)=C2OC3=NC=NC(N4CCN(CC4)[C@H](C5=CC=C(C=C5)F)C)=C3)=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
-
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.
-
Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
-
Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)