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

nor-Binaltorphimine  (Synonyms: Norbinaltorphimine; NorBNI)

製品番号: HY-117040 純度: 98.70%
COA 取扱説明書 Technical Support

nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

nor-Binaltorphimine

nor-Binaltorphimine 構造式

CAS 番号 : 105618-26-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 138 在庫あり
Solution
10 mM * 1 mL in DMSO USD 138 在庫あり
Solid
5 mg $95 在庫あり
10 mg $150 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of nor-Binaltorphimine:

nor-Binaltorphimine 関連抗体

Top Publications Citing Use of Products

Opioid Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain[1][2][3].

IC50 & Target[1]

κ Opioid Receptor/KOR

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.039 Ke/nM
Compound: nor BNI
Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.
Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.
[PMID: 12672258]
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 EC50
18.9 Ke/nM
Compound: nor BNI
Stimulation of DAMGO binding in recombinant human Opioid receptor mu 1 transfected into CHO cells
Stimulation of DAMGO binding in recombinant human Opioid receptor mu 1 transfected into CHO cells
[PMID: 12672258]
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 EC50
4.42 Ke/nM
Compound: nor BNI
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
Stimulation of [35S]GTP-gamma-S, binding at human recombinant Opioid receptor delta 1 transfected into CHO cells.
[PMID: 12672258]
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]
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 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 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]
HEK293 EC50
158 nM
Compound: NorBNI
Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor
Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor
[PMID: 17702750]
HEK293 IC50
2.1 nM
Compound: nor-BNI 1
Antagonist activity at human kappa opioid receptor expressed in HEK cells assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding
Antagonist activity at human kappa opioid receptor expressed in HEK cells assessed as inhibition of dynorphin A-induced [35S]GTPgammaS binding
[PMID: 20719509]
HEK293 IC50
212 nM
Compound: nor-BNI 1
Antagonist activity at human mu opioid receptor expressed in HEK cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding
Antagonist activity at human mu opioid receptor expressed in HEK cells assessed as inhibition of DAMGO-induced [35S]GTPgammaS binding
[PMID: 20719509]
HEK293 IC50
24 nM
Compound: nor-BNI 1
Antagonist activity at human delta opioid receptor expressed in HEK cells assessed as inhibition of SNC-80-induced [35S]GTPgammaS binding
Antagonist activity at human delta opioid receptor expressed in HEK cells assessed as inhibition of SNC-80-induced [35S]GTPgammaS binding
[PMID: 20719509]
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]
体外実験

Nor-binaltorphimine (0.01 nM-0.1 μM; 120 min) displaces the binding of [3H]U-69,593 to κ-opioid receptors in rat cortical cell membranes. Its Ki value is 4.8 nM in saline-infused rats, while its potency increases 12-fold (Ki = 0.4 nM) in butorphanol-infused rats, indicating that κ-opioid receptors are hypersensitive to this antagonist[2].
nor-Binaltorphimine (20-200 nM; 30 min) potently antagonizes κ-selective agonists in the longitudinal muscle of guinea pig ileum, while it exhibits extremely weak antagonistic effects on the μ-selective agonist morphine, with a κ/μ selectivity ratio of 19.2[3].
nor-Binaltorphimine (20 nM; 30 min) potently antagonizes κ-selective agonists in rabbit vas deferens preparations[3].

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

nor-Binaltorphimine 関連抗体
体内実験

Nor-binaltorphimine (30 μg; intracerebroventricular injection; single administration / twice daily; consecutive 10 days) acts as a selective, long-acting κ-opioid receptor antagonist in rats[1].
Nor-binaltorphimine (12-100 nM/5 μl; intracerebroventricular injection; administered twice, at 3 hours before and 48 hours after the initiation of butorphanol infusion) blocks most naloxone-precipitated withdrawal symptoms in butorphanol-dependent rats, exerts a significant blocking effect on diarrhea, alleviates forepaw tremor, and prevents butorphanol-induced desensitization of κ-opioid receptors in the cortex and striatum, as well as receptor downregulation in the cortex[2].

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

Animal Model: Sprague-Dawley (male, 250-270 g)[1]
Dosage: 30 μg (single treatment); 30 μg (repeated treatment)
Administration: i.c.v.; single injection (single treatment); i.c.v.; twice daily; 10 days (repeated treatment)
Result: Abolished U69593-induced antinociception (significant reduction in % MPE vs vehicle) when tested 1, 11, and 30 days post-single 30 μg i.c.v. injection.
Did not alter DAMGO- or DPDPE-induced antinociception when tested 1 and 11 days post-single 30 μg i.c.v. injection.
Abolished U69593-induced antinociception (significant reduction in % MPE vs vehicle) when tested 1, 2, 5, and 20 days post-last repeated 30 μg i.c.v. twice-daily injection.
Abolished DAMGO- and DPDPE-induced antinociception (significant reduction in % MPE vs vehicle) when tested 1 and 2 days post-last repeated 30 μg i.c.v. twice-daily injection.
Showed no effect on DAMGO- or DPDPE-induced antinociception at 5 and 20 days post-last repeated 30 μg i.c.v. twice-daily injection.
Exhibited magnitude of DAMGO and DPDPE antagonism on day 1 post-last repeated dose equivalent to that of selective μ-antagonist CTOP and δ-antagonist ICI 174,864, respectively.
Animal Model: Sprague-Dawley (7- to 8-week-old male, 250-300 g, butorphanol dependence model via intracerebroventricular osmotic minipump infusion of butorphanol tartrate at 26 nmol/h for 3 days)[2]
Dosage: 12 nM/5 μl per rat; 24 nM/5 μl per rat; 48 nM/5 μl per rat; 100 nM/5 μl per rat
Administration: i.c.v.; 2 doses (3 h before and 48 h after butorphanol infusion start)
Result: Completely blocked naloxone-precipitated withdrawal signs of escape behavior, teeth-chattering, wet shakes, ptosis, body weight loss (>3%), and reversed hypothermia to increased rectal temperatures.
Significantly blocked diarrhea at 12 nM dose.
Significantly blocked diarrhea and attenuated forepaw tremors at 24 nM dose.
Had no effect on withdrawal signs of yawning, ejaculation, or urination.
Prevented butorphanol-induced increases in [3H]U-69,593 K_D values in the cortex (4.33 nM, 96% of saline control) and striatum (5.49 nM, 105% of saline control) at 12 nmol dose.
Prevented butorphanol-induced decreases in [3H]U-69,593 B_max values in the cortex (59.46 fM/mg protein, 97% of saline control) at 12 nmol dose.
Prevented butorphanol-induced supersensitivity of cortical κ-opioid receptors to nor-binaltorphimine itself, blocking the significant reduction in K_i values seen with butorphanol alone.
分子量

661.79

分子式

C40H43N3O6
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (151.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

*"≥" means soluble, but saturation unknown.

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
10 mM 0.1511 mL 0.7555 mL 1.5111 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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).
純度とドキュメンテーション
参考文献

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 / DMSO 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
DMSO 50 mM 0.0302 mL 0.1511 mL 0.3022 mL 0.7555 mL
60 mM 0.0252 mL 0.1259 mL 0.2518 mL 0.6296 mL
80 mM 0.0189 mL 0.0944 mL 0.1889 mL 0.4722 mL
100 mM 0.0151 mL 0.0756 mL 0.1511 mL 0.3778 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

nor-Binaltorphimine Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

nor-Binaltorphimine105618-26-6Norbinaltorphimine NorBNIOpioid Receptorκ-opioid receptorδ-opioid receptorbutorphanol dependencerabbit vas deferensratsmouse vas deferensμ-opioid receptorguinea pig ileal longitudinal muscledynorphin 1-17rat cortical membranesInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
nor-Binaltorphimine
製品番号:
HY-117040
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.