2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. Oveporexton

Oveporexton (TAK-861) is an orally active and selective orexin receptor 2 (OX2R) agonist with an EC50 of 2.5 nM. Oveporexton exhibits 3000-fold selectivity for OX2R over OX1R. Oveporexton can be used for the study of hypersomnia disorders including narcolepsy.

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Oveporexton

Oveporexton 화학구조

CAS No. : 2460722-04-5

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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Oveporexton Related Antibodies

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OX2 Receptor OX1 Receptor

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Oveporexton (TAK-861) is an orally active and selective orexin receptor 2 (OX2R) agonist with an EC50 of 2.5 nM. Oveporexton exhibits 3000-fold selectivity for OX2R over OX1R. Oveporexton can be used for the study of hypersomnia disorders including narcolepsy[1][2].

IC50 & Target[2]

OX2 Receptor

2.5 nM (EC50)

OX1 Receptor

7500 nM (EC50)

In Vitro

Oveporexton potently activates recombinant OX2R (EC50 of 2.5 nM) and weakly activates OX1R (EC50 of 7500 nM)[2].
Oveporexton (10-1000 nM) induces dose-dependent depolarization of the membrane potential in histaminergic neurons in the mouse tuberomammillary nucleus with an EC50 of 31.7 nM[2].

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

Oveporexton Related Antibodies
In Vivo

Oveporexton (0.03-10 mg/kg; p.o.) improves narcolepsy-like phenotype in mice, significantly increasing total waking time[2].
Oveporexton (1 mg/kg; p.o.) significantly increases wakefulness time in cynomolgus monkeys[2].

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

Animal Model: Male C57BL/6J mice (3 weeks old for slice electrophysiology), male OX2R KO mice (18 weeks old), male orexin/ataxin-3 mice and their WT littermates (22-29 weeks old)[2]
Dosage: For WT mice: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg; For OX2R KO mice: 10 mg/kg; For orexin/ataxin-3 mice: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration: Oral administration; single dose for most experiments, except for the repeated administration study in orexin/ataxin-3 mice where it was administered once daily for 14 days in the sub-chronic treatment group
Result: Increased total wakefulness time and decreased NREM and REM sleep times (in WT mice).
Had no effect on sleep-wake parameters (in OX2R KO mice).
Increased wakefulness, decreased NREM sleep, improved wakefulness fragmentation, and reduced cataplexy -like episodes (in orexin/ataxin-3 mice).
Clinical Trial
분자량

520.51

화학식

C23H25F5N2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(O)C(N(CC(F)([C@@H]1NS(CC)(=O)=O)F)[C@H]1CC2=C(C(C3=CC(F)=CC(F)=C3)=CC=C2)F)=O
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

DMSO : 50 mg/mL (96.06 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 1.9212 mL 9.6060 mL 19.2119 mL
5 mM 0.3842 mL 1.9212 mL 3.8424 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 5 mg/mL (9.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (9.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
순도&문서
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 1.9212 mL 9.6060 mL 19.2119 mL 48.0298 mL
5 mM 0.3842 mL 1.9212 mL 3.8424 mL 9.6060 mL
10 mM 0.1921 mL 0.9606 mL 1.9212 mL 4.8030 mL
15 mM 0.1281 mL 0.6404 mL 1.2808 mL 3.2020 mL
20 mM 0.0961 mL 0.4803 mL 0.9606 mL 2.4015 mL
25 mM 0.0768 mL 0.3842 mL 0.7685 mL 1.9212 mL
30 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6010 mL
40 mM 0.0480 mL 0.2401 mL 0.4803 mL 1.2007 mL
50 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9606 mL
60 mM 0.0320 mL 0.1601 mL 0.3202 mL 0.8005 mL
80 mM 0.0240 mL 0.1201 mL 0.2401 mL 0.6004 mL
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Oveporexton 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:

Oveporexton2460722-04-5TAK-861TAK861TAK 861Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT Receptormiceorexin/ataxin-3 micenarcolepsy-likewaking timeInhibitorinhibitorinhibit

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상품명:
Oveporexton
Cat. No.:
HY-159835
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