2. GPCR/G Protein Immunology/Inflammation
  3. GnRH Receptor Nuclear Factor of activated T Cells (NFAT)
  4. (R)-Elagolix

(R)-Elagolix  (Synonyms: NBI-56418)

製品番号: HY-14789 純度: 96.05%
COA 取扱説明書 Technical Support

Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

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(R)-Elagolix

(R)-Elagolix 構造式

CAS 番号 : 834153-87-6

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 83 在庫あり
Solution
10 mM * 1 mL in DMSO USD 83 在庫あり
Solid
5 mg $60 在庫あり
10 mg $90 在庫あり
25 mg $180 在庫あり
50 mg $290 在庫あり
100 mg $460 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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(R)-Elagolix 関連抗体

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製品説明

Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (KD = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. [1][2][3][4][5].

IC50 & Target

GnRHR

0.25 nM (IC50)

NFAT

5.4 nM (IC50)

体外実験

Elagolix is a human GnRH receptor (GnRHR) antagonist, with an IC50 of 0.25 nM in kinase assays[1].
Elagolix also shows NFAT inhibitory effects, with an IC50 of 5.4 nM, and effectively blocks Ca2+ flux, with an IC50 of 0.86 nM[1].
Elagolix is a human GnRH receptor (GnRHR) antagonist, with a Ki value of 3.7 nM[2].

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

(R)-Elagolix 関連抗体
体内実験


Main pharmacokinetic parameters after taking a single oral dose of elagolix to rats[3]

Route Dose (mg/kg) AUC0→t (ng•h/mL) AUC0→∞ (ng•h/mL) t1/2 (h) Tmax (h) Cmax (ng/mL)
Oral 15 5212 5301 6.56 1.50 1515

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

631.59

分子式

C32H30F5N3O5
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

FC1=C(C2=C(C)N(CC3=C(C(F)(F)F)C=CC=C3F)C(N(C[C@](C4=CC=CC=C4)([H])NCCCC(O)=O)C2=O)=O)C=CC=C1OC
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 62.5 mg/mL (98.96 mM; ultrasonic and warming and heat to 60°C; 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 1.5833 mL 7.9165 mL 15.8331 mL
5 mM 0.3167 mL 1.5833 mL 3.1666 mL
10 mM 0.1583 mL 0.7917 mL 1.5833 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
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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

体内:

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 (3.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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 (3.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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:

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.
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.
純度とドキュメンテーション

純度: 96.05%

COA (251 KB) HNMR (329 KB) LCMS (98 KB)

取扱説明書 (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5833 mL 7.9165 mL 15.8331 mL 39.5826 mL
5 mM 0.3167 mL 1.5833 mL 3.1666 mL 7.9165 mL
10 mM 0.1583 mL 0.7917 mL 1.5833 mL 3.9583 mL
15 mM 0.1056 mL 0.5278 mL 1.0555 mL 2.6388 mL
20 mM 0.0792 mL 0.3958 mL 0.7917 mL 1.9791 mL
25 mM 0.0633 mL 0.3167 mL 0.6333 mL 1.5833 mL
30 mM 0.0528 mL 0.2639 mL 0.5278 mL 1.3194 mL
40 mM 0.0396 mL 0.1979 mL 0.3958 mL 0.9896 mL
50 mM 0.0317 mL 0.1583 mL 0.3167 mL 0.7917 mL
60 mM 0.0264 mL 0.1319 mL 0.2639 mL 0.6597 mL
80 mM 0.0198 mL 0.0990 mL 0.1979 mL 0.4948 mL
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(R)-Elagolix 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:

(R)-Elagolix834153-87-6NBI-56418NBI56418NBI 56418GnRH ReceptorNuclear Factor of activated T Cells (NFAT)Gonadotropin releasing hormone receptorGNRHRCan be taken orallymesenteriorrheaInhibitorinhibitorinhibit

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製品番号:
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