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Art. -Nr.: HY-178720

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SHR0687

SHR0687 is a selective tetrapeptide kappa opioid receptor (KOR) agonist with an EC₅₀ of 0.53 pM. SHR0687 displays high potency and selectivity over MOR and DOR, with negligible blood-brain barrier penetration. SHR0687 activates KOR specifically, leading to potential modulation of neurological pathways without significant central nervous system effects. SHR0687 can be used for the research of pain.

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CAS. Nr.: 2168573-03-1
Formel: C₃₉H₆₀N₈O₅
Molecular Weight:720.94

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

SHR0687 Chemical Structure

CAS. Nr.: 2168573-03-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

κ Opioid Receptor/KOR

0.53 pM (EC₅₀)

μ Opioid Receptor/MOR

>50000 nM (EC₅₀)

δ Opioid Receptor/DOR

>50000 nM (EC₅₀)

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

SHR0687 (Human embryonic kidney cells (HEK293)) does not inhibit hERG channels^[1].
SHR0687 (Human liver microsomes) does not significantly inhibit major CYP isoforms, including CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	T_1/2	Clearance (CL)	V_z	AUC_0-t
Rat^[1]	1 mg/kg	i.v.	4.78 h	10.5 mL/min/kg	4515 mL/kg	1553 ng·h/mL
Mice^[1]	1 mg/kg	i.v.	0.34 h	10.1 mL/min/kg	297 mL/kg	1656 ng·h/mL
Dog^[1]	0.5 mg/kg	i.v.	4.45 h	3.1 mL/min/kg	1236 mL/kg	2619 ng·h/mL

In Vivo

SHR0687 (0.03-0.3 mg/kg; Intravenous (IV); once) demonstrates analgesic effects in carrageenan-induced pain model in Sprague Dawley rats (SD)^[1].
SHR0687 (1 mg/kg; Intravenous (IV); administration) shows minimal BBB penetration in Sprague Dawley rats (SD)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague Dawley rats (SD) (150-180 g) were subcutaneously injected with 1% carrageenan (100 μL)^[1]
Dosage:

0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg
Administration:

i.v.;30 minutes before detection
Result:

A dose-dependent reduction in pain was observed.

Chemical Information

CAS. Nr. 2168573-03-1
Molecular Weight 720.94
Formel C₃₉H₆₀N₈O₅
SMILES

C[C@H](C1=CC=CC=C1)CNCC(N[C@H](CC2=CC=CC=C2)C(N[C@H](CC(C)C)C(N[C@H](CCCCN)C(N3CCC(CC3)NC(NC)=O)=O)=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Li X, et al. Discovery of SHR0687, a Highly Potent and Peripheral Nervous System-Restricted KOR Agonist. ACS Med Chem Lett. 2020;11(11):2151-2155. Published 2020 Sep 14. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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SHR0687

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

SHR0687 Related Classifications

HY-178720 Related Classifications