MM 54( —— )

Catalog No. M30643 CAS No. 1313027-43-8

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Datasheet

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Product Name

MM 54
Note

Research use only, not for human use.
Brief Description

Potent apelin receptor antagonist (Ki = 82 nM; IC50 = 93 nM). Antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells. Recuces tumor expansion and lengthens survival time in a mouse xenograft model of glioblastoma.
Description

Potent apelin receptor antagonist (Ki = 82 nM; IC50 = 93 nM). Antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells. Recuces tumor expansion and lengthens survival time in a mouse xenograft model of glioblastoma.
In Vitro

MM 54 inhibits more than 95% of apelin binding to APLNR at the dose of 10 μM.
In Vivo

MM 54 (2 mg/kg, ip, bi-weekly for 4 weeks) possesses anti-tumor activity in glioblastoma models with no obvious toxicity. Animal Model:Tumour-bearing nude-mice.Dosage:2 mg/kg.Administration:Intraperitoneal injection, bi-weekly for 4 weeks.Result:Reduced tumor progression (glioblastoma).
Synonyms

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Pathway

Others
Target

Other Targets
Recptor

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Research Area

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Indication

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CAS Number

1313027-43-8
Formula Weight

1737.15
Molecular Formula

C70H121N29O15S4
Purity

>98% (HPLC)
Solubility

water:2 mg/mL
SMILES

[H]N[C@H]1CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(N)=N)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(N)=N)NC1=O)C(O)=O
Chemical Name

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1. Macaluso et al (2011) Discovery of a competitive apelin receptor (APJ) antagonist. ChemMedChem 6 1017 PMID:

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