2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. 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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SHR0687

SHR0687 화학구조

CAS No. : 2168573-03-1

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SHR0687 Related Antibodies

Top Publications Citing Use of Products

View All Opioid Receptor Isoform Specific Products:

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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • 순도&문서

  • References

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제품 설명

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[1].

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)

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.

SHR0687 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Clearance (CL) Vz AUC0-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.
분자량

720.94

화학식

C39H60N8O5
CAS No.
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
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
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SHR0687 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SHR06872168573-03-1SHR 0687SHR-0687Opioid Receptoropioid receptorsKOR agonistperipheral KOR activationcarrageenan-induced pain modelInhibitorinhibitorinhibit

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상품명:
SHR0687
Cat. No.:
HY-178720
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