1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. nor-Binaltorphimine

nor-Binaltorphimine  (Synonyms: Norbinaltorphimine; NorBNI)

Cat. No.: HY-117040 Purity: 98.20%
SDS COA Handling Instructions

nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo.

For research use only. We do not sell to patients.

nor-Binaltorphimine Chemical Structure

nor-Binaltorphimine Chemical Structure

CAS No. : 105618-26-6

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1 mg USD 150 In-stock
5 mg USD 380 Get quote
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of nor-Binaltorphimine:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

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Description

nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo[1].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.28 nM
Compound: norBNI
Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
[PMID: 25593096]
CHO EC50
120 nM
Compound: 1, norBNI
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 20568781]
CHO IC50
2.9 nM
Compound: norBNI
Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
Antagonist activity at mouse kappa opioid receptor-1 expressed in CHO cell membranes assessed as inhibition of U50,488H-induced [35S]GTPgammaS binding incubated for 60 mins by scintillation spectroscopic analysis
[PMID: 27556704]
CHO EC50
380 nM
Compound: 1, norBNI
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 20568781]
CHO IC50
4.6 nM
Compound: norBNI
Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced ERK phosphorylation pre-incubated with compound before U69,593 stimulation for 10 mins
Antagonist activity against HA-tagged human recombinant kappa opioid receptor expressed in CHO cells assessed as inhibition of U69,593-induced ERK phosphorylation pre-incubated with compound before U69,593 stimulation for 10 mins
[PMID: 25593096]
CHO EC50
6 nM
Compound: 1, norBNI
Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 20568781]
U2OS IC50
2.5 nM
Compound: norBNI
Antagonist activity against human kappa opioid receptor expressed in human U2OS cells co-expressing beta-arrestin2 pre-treated for 15 mins before U69,593 stimulation for 90 mins by DiscoveRx beta-arrestin2 recruitment based PathHunter assay
Antagonist activity against human kappa opioid receptor expressed in human U2OS cells co-expressing beta-arrestin2 pre-treated for 15 mins before U69,593 stimulation for 90 mins by DiscoveRx beta-arrestin2 recruitment based PathHunter assay
[PMID: 25593096]
Molecular Weight

661.79

Formula

C40H43N3O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@]12[C@]34[C@](OC5=C(O)C=CC(C[C@@]2([H])N(CC4)CC6CC6)=C53)([H])C7=C(C8=C([C@@]9([H])[C@]%10%11[C@@](C8)([C@](CC%12=C%11C(O9)=C(C=C%12)O)([H])N(CC%10)CC%13CC%13)O)N7)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 33.08 mg/mL (49.99 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5111 mL 7.5553 mL 15.1105 mL
5 mM 0.3022 mL 1.5111 mL 3.0221 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 98.20%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.5111 mL 7.5553 mL 15.1105 mL 37.7763 mL
5 mM 0.3022 mL 1.5111 mL 3.0221 mL 7.5553 mL
10 mM 0.1511 mL 0.7555 mL 1.5111 mL 3.7776 mL
15 mM 0.1007 mL 0.5037 mL 1.0074 mL 2.5184 mL
20 mM 0.0756 mL 0.3778 mL 0.7555 mL 1.8888 mL
25 mM 0.0604 mL 0.3022 mL 0.6044 mL 1.5111 mL
30 mM 0.0504 mL 0.2518 mL 0.5037 mL 1.2592 mL
40 mM 0.0378 mL 0.1889 mL 0.3778 mL 0.9444 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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nor-Binaltorphimine Related Classifications

Help & FAQs
  • 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.

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nor-Binaltorphimine
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