PL-3994
PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. PL-3994 produces concentration-dependent relaxation of pre-contracted guinea-pig trachea with an IC50 value of 42.7 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 952295-80-6
- Formule: C82H127N27O20S2
- Masse moléculaire:1875.18
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
PL-3994 has high affinity for recombinant human, dog, or rat NPR-As with Ki values of 1 nM, 41 nM, 10 nM, respectively. And PL-3994 binds to hNPR-C with Ki of 7 nM, while there is no effect on cGMP generation in hNPR-B[1].
PL-3994 induces dose-dependent cGMP generation in human, dog, and rat NPR-As with EC50s of 2 nM, 3 nM, and 14 nM, respectively[1].
PL-3994 (0.1 nM-100 mM; 5-20 min) elicits a potent, concentration-dependent but small relaxation of pre-contracted human precision-cut lung slices (hPCLS)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PL-3994 is resistant to degradation by human neutral endopeptidase (hNEP) (92% remaining after 2 h), whereas the natural ligands, ANP and CNP, are rapidly metabolized (≤1% remaining after 2 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Guinea-pig model anaesthetized with urethane (1.75 g/kg, i.p.)[1]
-
Dosage:1, 10, 100, 1000 mg/kg
-
Administration:Intrathecal; single dose
-
Result:Resulted a significant maximum inhibition of 43%, 63% and 70%, respectively, observed after 15-min pretreatment at doses of 10, 100 and 1000 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 952295-80-6
-
Masse moléculaire 1875.18
-
Formule C82H127N27O20S2
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Edelson JD, et al. In vitro and in vivo pharmacological profile of PL-3994, a novel cyclic peptide (Hept-cyclo(Cys-His-Phe-d-Ala-Gly-Arg-d-Nle-Asp-Arg-Ile-Ser-Cys)-Tyr-[Arg mimetic]-NH(2)) natriuretic peptide receptor-A agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. Pulm Pharmacol Ther. 2013 Apr;26(2):229-38. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PL-3994 Related Classifications
HY-P3562 Related Classifications
Powered by Bioz