U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 221 - 230 of 2596 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Epilovastatin is a Lovastatin impurity (Simvastatin Impurity F).
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

TCS-OX2-29 is a potent and selective orexin-2 (OX2) receptor antagonist, displaying selectivity for OX2 over OX1. Also was shown, that TCS-OX2-29 inhibited orexin A induced inositol phosphate accumulation and ERK-1/2 phosphorylation in CHO cells stably expressing the OX2 receptor.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

TC OT 39 was developed as potent non-peptide oxytocin receptor partial agonist and V2 vasopressin receptor agonist. Also was a V1a vasopressin receptor antagonist.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Pyrabactin is a synthetic sulfonamide that functions both as selective ABA receptor agonist and antagonist. Abscisic acid (ABA) is an endogenous small molecule growth inhibitor and regulator of plant stress physiology. Pyrabactin mimics abscisic acid (ABA). It acts through Pyrabactin Resistance 1 (PYR1), the founding member of a family of START proteins called PYR/PYLs, which are necessary for both pyrabactin and ABA signaling in vivo. Pyrabactin an important tool for protecting crops against drought and cold weather.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

2-Epi-moxidectin is a degradation product of moxidectin, formed in a reaction with alkali. The compound may present as an impurity in moxidectin preparation.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

VU 10010 is a selective allosteric potentiator of M4 acetylcholine receptors. VU 10010 had no agonist, antagonist or allosteric potentiator activity at P2Y1R or mGluR5. VU 10010 is selective for M4 relative to other mAChRs - this compound does not displace [3H]NMS binding at any (rM1, rM2, rM3 and rM5) mAChR subtype. VU10010 was not found to be centrally active. It suffers from poor physiochemical properties. Novel analogs of VU10010 are CNS penetrant following systemic administration.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 uM, exhibits >500-fold selectivity over CYP3A5 and CYP3A7. PF-4981517 is a very useful tool for understanding the relative roles of CYP3A4 versus CYP3A5 and the impact of CYP3A5 genetic polymorphism on a compound's pharmacokinetics.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

DB07268, a 4-anilinopyrimidine compound, is an inhibitor of c-Jun N-terminal kinase (JNK1).
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

SR-57227A is a potent and selective agonist at the 5HT3 receptor, with high selectivity over other serotonin receptor subtypes and good blood-brain barrier penetration. SR-57227A had affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes in vitro. SR 57227A stimulated the uptake of [14C]guanidinium into NG 108-15 cells in the presence of substance P and contracted the isolated guinea-pig ileum, effects that were antagonized by the 5-H 3 receptor antagonist tropisetron. The agonist effect of SR 57227A was also observed in vivo, as the compound elicited the Bezold-Jarisch reflex in anesthetized rats, an effect that was blocked by tropisetron.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

AAL993 (ZK260253) is a potent and selective VEGF receptor kinase (VEGF-R) tyrosine kinase inhibitor (VEGFR2), which binds to an inactive conformation of the protein. In addition, AAL993 possesses dual functions, including suppression of HIF-1 alpha expression through ERK inhibition without affecting Akt phosphorylation.