RS-127445 - Moligand™, 10mM in DMSO , Antagonist of 5-HT 2A receptor;Antagonist of 5-HT 2B receptor;Antagonist of 5-HT 2C receptor, CAS No.199864-87-4, Antagonist of 5-HT 2A receptor;Antagonist of 5-HT 2B receptor;Antagonist of 5-HT 2C receptor

CAS: 199864-87-4 Cat. No.: R407929 Summenformel: C₁₇H₁₆FN₃ Molekulargewicht: 281.34 PubChem CID: 196968

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

MT500 | 4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

RS-127445 (MT500) is a selective5-HT2Breceptor antagonist withpKiof 9.5 andpIC50of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.
In vitro

RS-127445 is a novel high affinity, selective 5-HT2B receptor antagonist devoid of detectable intrinsic activity. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor. RS-127445 is thus among the highest affinity, most selective 5- HT2B receptor ligands. RS-127445 potently blocks the 5-HT evoked increase in inositol phosphate formation and blocks the 5-HT evoked increases in intracellular calcium concentrations with a potency 1000 times greater than that of yohimbine. ^[1]

In vivo

RS-127445 is readily absorbed with no obvious dose or route-dependent limitations and rapidly absorbed following both oral and intraperitoneal administration with peak plasma concentrations being achieved within 15 min of dosing. RS-127445 concentration in the plasma are proportional to the administered dose. RS-127445 administrated at dose of 5 mg/kg with approximately 60% of an intraperitoneal dose and 14% of the oral dose is bioavailable. RS-127445 concentration in the plasma is predicted to fully saturate accessible 5-HT2B receptors can be readily achieved and maintained in the rat. RS-127445 administered at 1 to 10 mg/kg with oral significantly inhibits visceral hypersensitivity up to 35 to 74% provoked by restraint stress. Oral RS-127445 produces a significant suppression of TNBS-induced visceral hypersensitivity (15 to 62% inhibition at 3 to 30 mg/ kg), although RS-127445 has no significant effect on the visceral nociceptive threshold of native rats. RS-127445 administrated orally with 1 to 30 mg/kg also dose -dependently reduce the restraint stress-induced defecation in native and TNBS-treated rats. ^[2]. RS-127445 inhibits colonic motility and defecation. ^[3]
Cell Data

cell lines：

Concentrations：10 μM

Incubation Time：20 min

Powder Purity:≥97%

Specifications

Synonyme

MT500 | 4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pK_i of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

ANTAGONIST

Mechanismus der Wirkung

Antagonist of 5-HT 2A receptor;Antagonist of 5-HT 2B receptor;Antagonist of 5-HT 2C receptor

Namen und Kennungen

Isomere SMILES

CC(C)C1=NC(=NC(=C1)C2=CC=C(C3=CC=CC=C32)F)N

Alternative CAS-Nummer

199864-87-4

PubChem CID

196968

MeSH-Eintrag

2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine;MT 500;MT-500;MT500 cpd;RS 127445;RS 27354;RS-127445;RS-27354;RS127445;RS27354

Molekulargewicht

281.34

Zugehörige Ziele (menschlich)

HTR1B Tclin 5-hydroxytryptamine receptor 1B (0 Activities)

Discover Target: HTR1B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2A Tclin 5-hydroxytryptamine receptor 2A (1 Activities)

Discover Target: HTR2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2C Tclin 5-hydroxytryptamine receptor 2C (1 Activities)

Discover Target: HTR2C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B (0 Activities)

Discover Target: HTR2B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro DMSO: 36 mg/mL (197.61 mM); Water: 36 mg/mL (197.61 mM); Ethanol: Insoluble