RLX-33 - ≥99% , CAS No.2784577-71-3

CAS: 2784577-71-3 Cat. No.: R650531 분자식: C₂₄H₁₉ClN₄O₄ 분자량: 462.89

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

개요

RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC 50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome

In Vivo

RLX-33 (10 mg/kg; IP, single dosage) attenuates the RXFP3-selective agonist R3/I5-induced increase in feeding in male Wistar rats . RLX-33 (10 mg/kg; IP, single dosage) exhibits a good brain penetration and highly protein-bound in rats plasma . Pharmacokinetic Parameters of RLX-33 in male Wistar rats (IP, 10 mg/kg) . plasma brain C max (ng/mL) 1401 1552 t max (h) 0.5 2.0 t 1/2 (h) 1.9 4.9 AUC inf (ng/mL·h) 5352 12519 CL_F (mL/min/kg) 43.8 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar rats (intracerebroventricular administration of R3/I5 stimulated food intake Dosage: 10 mg/kg Administration: IP, single dosage Result: Attenuated the R3/I5-induced increase in food intake. Animal Model: Male Wistar rats Dosage: 10 mg/kg Administration: IP, single dosage (Pharmacokinetic Analysis) Result: Exhibited a good brain penetration and highly protein-bound, with protein binding of 99.8% in rat plasma.

Form:Solid

IC50& Target:IC 50 : 2.36 μM (RXFP3), 7.82 μM (ERK1 phosphorylation), 13.86 μM (ERK2 phosphorylation)

Specifications

사양 및 순도

≥99%

생화학 및 생리적 메커니즘

RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC 50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphoryl

보관 조건

Store at -20°C

배송

Ice chest + Ice pads

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순수함

≥99%

이름과 식별자

• 분자량: 462.89

화학 및 물리적 특성

• 용해성: DMSO : 125 mg/mL (270.04 mM; Need ultrasonic)