Loperamide HCl - 10mM in DMSO , Mu opioid receptor agonist, CAS No.34552-83-5, Mu opioid receptor agonist

CAS: 34552-83-5 Cat. No.: L408678 Fórmula: C₂₉H₃₃ClN₂O₂·HCl Peso molecular: 513.5 Número EC: 252-082-4

GRADE & PURITY 10mM in DMSO

Synonyms

ADL 2-1294 | 4-​(4-​chlorophenyl)​-​4-​hydroxy-​N,​N-​dimethyl-​α,​α-​diphenyl-1-​piperidinebutanamide​, hydrochloride (1:1)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Loperamide HCl (ADL 2-1294) is a selectiveμ-opioid receptoragonist opioid withKiof 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bow
In vitro

Loperamide exhibits potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently stimulates [³⁵S]guanosine-5\'-O-(3-thio)triphosphate binding with EC50 of 56 nM, and inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide potently inhibits late-phase formalin-induced flinching after intrapaw injection (A50 = 6 mg). Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC50 = 0.44 mM). Loperamide reversibly blocks rises in [Ca2+]i evoked by high [K+] in a concentration-dependent manner, with an IC50 of 0.9 mM. Loperamide (0.1-50 mM) produces a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM and, at the highest concentration tested, could fully block IBa in the absence of any other pharmacological agent. Loperamide also attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV, with an IC50 of 73 mM.

In vivo

Loperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia when s.c. injected, locally over the tibial tumoral mass (7.5-75 mg) or distantly, under the fur of the neck (4 mg/kg) in mice.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

ADL 2-1294 | 4-​(4-​chlorophenyl)​-​4-​hydroxy-​N,​N-​dimethyl-​α,​α-​diphenyl-1-​piperidinebutanamide​, hydrochloride (1:1)

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Loperamide HCl (ADL 2-1294) is a selective μ-opioid receptor agonist opioid with K_i of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or i

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

AGONIST

Mecanismo de acción

Mu opioid receptor agonist

Nombres e identificadores

• Isómeros SMILES: CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl
• WGK Alemania: 3
• RTECS: TM4960000
• Peso molecular: 513.5
• Reaxy-Rn: 4087090
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4087090&ln=

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 82 mg/mL (199.08 mM); Water: 82 mg/mL (199.08 mM); Ethanol: 82 mg/mL (199.08 mM)
• Punto de fusión (°C): 223°C

Preguntas frecuentes

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 34552-83-5, the molecular formula is C29H34Cl2N2O2, and the molecular weight is 513.5 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.