2. GPCR/G Protein Cell Cycle/DNA Damage
  3. GnRH Receptor PERK
  4. NBI-42902

NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.

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

NBI-42902 Chemical Structure

NBI-42902 Chemical Structure

CAS No. : 352290-60-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 419 In-stock
Solution
10 mM * 1 mL in DMSO USD 419 In-stock
Solid
1 mg USD 174 In-stock
5 mg USD 384 In-stock
10 mg USD 615 In-stock
25 mg USD 1289 In-stock
50 mg USD 2062 In-stock
100 mg USD 3300 In-stock
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Based on 1 publication(s) in Google Scholar

NBI-42902 Related Antibodies

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  • Purity & Documentation

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Description

NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases[1].

In Vitro

NBI-42902 (0-1000 nM) is quite sensitive to the relatively conservative sequence changes between species, with IC50 values of 0.79 nM (human), 10 nM (macaque), 400 nM (dog), 200 nM (rabbit) for the GnRH receptors[1].
NBI-42902 (1 nM-1 μM, 1 min) inhibits GnRH (4 nM)-stimulated Ca2+ flux in RBL cells with a mean IC50 value of 3.6 nM[1].
NBI-42902 (1 nM-1 μM, 1 min) inhibits GnRH (4 nM)-induced IP accumulation competitively in RBL cells[1].
NBI-42902 (1 nM-1 μM, 5 min) blocks GnRH-stimulated ERK1/2 phosphorylation completely in CHO-GnRHR cells with an IC50 value of 5.22 nM[1].

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

NBI-42902 Related Antibodies

Western Blot Analysis[1]

Cell Line: CHO-GnRHR
Concentration: 1 nM-1 μM
Incubation Time: 5 min
Result: Blocked GnRH (1 nM)-stimulated ERK1/2 phosphorylation completely in a dose-dependent manner, with an IC50 value of 5.22 nM.
In Vivo

NBI-42902 (10-100 mg/kg, p.o. or i.v. ) inhibits serum LH levels significantly in castrated macaques[1].

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

Animal Model: Castrated macaques[1]
Dosage: 10, 40, 100 mg/kg
Administration: Oral administration (p.o.)
Result: Inhibited serum LH with dose dependent.
Inhibited serum LH achieved maximum suppression, that was 62-68% of pretreatment baseline, at 4-8 h after administration.
Exhibited no suppression of LH levels after 24 h treated with 10 or 40 mg/kg, but remained suppression at 100 mg/kg.
Animal Model: Castrated macaques[1]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.)
Result: Inhibited serum LH achieved maximum suppression was 62-68% of pretreatment baseline between 4-8 h after administration, but exhibited no suppression after 24 h.
Molecular Weight

495.49

Formula

C27H24F3N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C[C@H](N)C2=CC=CC=C2)C(C(C3=CC=CC(OC)=C3F)=C(C)N1CC4=C(F)C=CC=C4F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (201.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0182 mL 10.0910 mL 20.1820 mL
5 mM 0.4036 mL 2.0182 mL 4.0364 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)

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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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (5.05 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.05 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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
DMSO 1 mM 2.0182 mL 10.0910 mL 20.1820 mL 50.4551 mL
5 mM 0.4036 mL 2.0182 mL 4.0364 mL 10.0910 mL
10 mM 0.2018 mL 1.0091 mL 2.0182 mL 5.0455 mL
15 mM 0.1345 mL 0.6727 mL 1.3455 mL 3.3637 mL
20 mM 0.1009 mL 0.5046 mL 1.0091 mL 2.5228 mL
25 mM 0.0807 mL 0.4036 mL 0.8073 mL 2.0182 mL
30 mM 0.0673 mL 0.3364 mL 0.6727 mL 1.6818 mL
40 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2614 mL
50 mM 0.0404 mL 0.2018 mL 0.4036 mL 1.0091 mL
60 mM 0.0336 mL 0.1682 mL 0.3364 mL 0.8409 mL
80 mM 0.0252 mL 0.1261 mL 0.2523 mL 0.6307 mL
100 mM 0.0202 mL 0.1009 mL 0.2018 mL 0.5046 mL
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NBI-42902 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.

Keywords:

NBI-42902352290-60-9NBI42902NBI 42902GnRH ReceptorPERKGonadotropin releasing hormone receptorGNRHRProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseRBLoral activitycastrated macaquessex-hormone-related diseasesInhibitorinhibitorinhibit

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