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.
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- CAS No.: 952295-80-6
- Formule: C82H127N27O20S2
- Masse moléculaire:1875.18
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
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. Further protocols information, click here.
In Vivo
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.
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Animal Model:Guinea-pig model anaesthetized with urethane (1.75 g/kg, i.p.)[1]
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Dosage:1, 10, 100, 1000 mg/kg
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Administration:Intrathecal; single dose
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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.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 952295-80-6
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Masse moléculaire 1875.18
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Formule C82H127N27O20S2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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.
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
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