2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. SB-674042

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively.

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SB-674042

SB-674042 構造式

CAS 番号 : 483313-22-0

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 144 在庫あり
Solution
10 mM * 1 mL in DMSO USD 144 在庫あり
Solid
5 mg $131 在庫あり
10 mg $218 在庫あり
25 mg $500 在庫あり
50 mg $800 在庫あり
100 mg $1280 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 3 publication(s) in Google Scholar

Other Forms of SB-674042:

SB-674042 関連抗体

Top Publications Citing Use of Products

Orexin Receptor (OX 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
OX2 Receptor OX1 Receptor

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製品説明

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively[1][4].

IC50 & Target[1][4]

OX1 Receptor

3.76 nM (IC50)

OX2 Receptor

531 nM (IC50)

OX1 Receptor

1.1 nM (Ki)

OX2 Receptor

129 nM (Ki)

体外実験

SB-674042 ([3H]) (0.2-24 nM; 2 h) shows high-affinity and serves as a radio ligand suitable for labelling human OX1 receptors stably expressed in CHO cells[1].
SB-674042 (5 μM; 4 °C for 30 min, and 37 °C for 3 h) reduces the potency of CB1 receptor agonist (HY-14137) to phosphorylate ERK1/2 in HEK293 cells co-expressing the orexin-1 and CB1 receptors[2].
SB-674042 (1 μM; 24 h) eradicates the increase in mTOR phosphorylation in response to Orexin-A (HY-106224) (1 nM-1 μM; 24 h) in INS-1 cells, indicating activation of the mTOR pathway induced by orexin-A was dependent on the activated OX1 receptor[3].

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

SB-674042 関連抗体

Western Blot Analysis[3]

Cell Line: INS-1 cells
Concentration: 1 μM
Incubation Time: 24 hours; accompanied with 1 μM Orexin-A for 24 hour
Result: Decreased the phosphorylation level of mTOR induced by Orexin-A.
体内実験

SB-674042 (0.3 nM/0.3 μL; icv; single dose) reduces contextual and cues fear freezing responses in Stay animals in Stress Alternatives Model (SMA) in mice[4].

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

Animal Model: Stress-induced mice model (male C57BL/6NHsd mice, 22-26 g)[4]
Dosage: 0.3 nM/0.3 μL
Administration: Intracerebroventricular injection; subjected mice to 4 days of social aggression (days 1-4)
Result: Resulted 39.4% Escape and 60.6% Stay phenotypes among mice.
分子量

448.51

分子式

C24H21FN4O2S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

FC1=C(C2=C(C(N3[C@H](CC4=NN=C(C5=CC=CC=C5)O4)CCC3)=O)N=C(C)S2)C=CC=C1
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 : 25 mg/mL (55.74 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 2.2296 mL 11.1480 mL 22.2960 mL
5 mM 0.4459 mL 2.2296 mL 4.4592 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 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)

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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

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体積 （開始）

V1

=
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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: ≥ 1.43 mg/mL (3.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: ≥ 1.43 mg/mL (3.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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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mg/kg

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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 +
% 
+
%
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%
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
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 2.2296 mL 11.1480 mL 22.2960 mL 55.7401 mL
5 mM 0.4459 mL 2.2296 mL 4.4592 mL 11.1480 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 mL 5.5740 mL
15 mM 0.1486 mL 0.7432 mL 1.4864 mL 3.7160 mL
20 mM 0.1115 mL 0.5574 mL 1.1148 mL 2.7870 mL
25 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2296 mL
30 mM 0.0743 mL 0.3716 mL 0.7432 mL 1.8580 mL
40 mM 0.0557 mL 0.2787 mL 0.5574 mL 1.3935 mL
50 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
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SB-674042 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:

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製品番号:
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