CXCR7 modulator 2 - 10mM in DMSO , CAS No.2227426-37-9

CAS: 2227426-37-9 Cat. No.: C656467 Formula: C₂₉H₄₂N₆O₃ Peso molecolare: 522.68 PubChem CID: 134694953

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 ( CXCR7 ), with a K i of 13 nM.

In Vitro

CXCR7 modulator 2 (compound 18) demonstrates potent CXCR7-binding affinity (K i =13 nM) and β-arrestin activity (EC 50 =11 nM). CXCR7 modulator 2 also exhibits improved selectivity in the GPCR panel and an improved therapeutic index in the hERG patch-clamp assay in comparison with 11c. CXCR7 modulator 2 exhibits moderate to high in vitro turn over in both NADPH-supplemented mouse-liver microsomes (MLM, 93 μL/min/mg) and hepatocytes (28 μL/min per million cells), shows poor passive absorptive permeability in the MDCK II-permeability assay, and has good aqueous solubility. CXCR7 modulator 2 is rapidly absorbed with a mean maximal plasma concentration (C max ) of 682 ng/mL, which occurrs at 0.25 h (T max ). The corresponding mean area under the plasma-concentration-versus-time profile (AUC) is 740 ng/mL/h. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The administration of isoproterenol for 9 days leads to the development of cardiac fibrosis, as attested by the approximately 4-fold increase in collagen deposition relative to that in the control, which is detected by picrosirius-red staining. Treatment with CXCR7 modulator 2 results in a statistically significant reduction in cardiac fibrosis, thereby demonstrating the protective role of CXCR7 modulation with CXCR7 modulator 2 in an isoproterenol-induced cardiac injury . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:CXCR7 13 nM (Ki)

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 ( CXCR7 ), with a K i of 13 nM.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

MODULATOR

Nomi e identificatori

• Isomeri SMILES: CCC1=C(C2=NC=CN2C=C1)N3CCCN(CC3)[C@@H](CC(=O)N)C4CCN(CC4)C(=O)[C@H]5C[C@@H]6CC[C@H]5O6
• PubChem CID: 134694953
• Peso molecolare: 522.68

Obiettivi associati (umani)

ACKR3 Tchem Atypical chemokine receptor 3 (3 Activities)

Discover Target: ACKR3

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

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (1 Activities)

Discover Target: KCNH2

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

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2227426-37-9, the molecular formula is C29H42N6O3, and the molecular weight is 522.68 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.