2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. ACT-335827

ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders.

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ACT-335827 Chemical Structure

ACT-335827 Chemical Structure

CAS No. : 1354039-86-3

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Based on 1 publication(s) in Google Scholar

ACT-335827 Related Antibodies

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OX2 Receptor OX1 Receptor

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Description

ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders[1].

IC50 & Target[1]

OX1

6 nM (IC50)

OX2

417 nM (IC50)

In Vitro

ACT-335827 (0-10 μM, 2 h) acts on OXR-1 and OXR-2 with the Kb values of 41 nM and 560 nM, the IC50 values of 120 nM and 2300 nM, respectively in CHO cells[1].

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

ACT-335827 Related Antibodies
In Vivo

ACT-335827 (oral gavage, 30-100 mg/kg, once) can reduce the fear-induced startle response with no affecting motor or cognitive function in rats[1].
ACT-335827 (oral administration, 300 mg/kg, everyday, 4 weeks) has less effect on metabolic syndrome (MetS), such as diet-induced obesity (DIO) in male Wistar rats[2].

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

Animal Model: Rats[1]
Dosage: 30, 100 or 300 mg/kg
Administration: Oral gavage; once
Result: Reduced fear-induced startle response at 300 mg/kg.
Decreased stress-induced elevated body temperature at 300 mg/kg and accelerated heat rate at 100 or 300 mg/kg but no effect on locomotion and blood pressure.
Animal Model: Male Wistar rats weighing160-180g[2]
Dosage: 300 mg/kg
Administration: Oral administration; everyday; 4 weeks
Result: Reduced preference for high fat/sweet diets but no effect on absolute energy intake.
Increased water intake and HDL relative to total cholesterol.
Resulted in a 4% weight gain compared to the control group.
Molecular Weight

518.64

Formula

C31H38N2O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC1=C(OC)C=CC(C[C@H]2C3=CC(OC)=C(OC)C=C3CCN2[C@H](C4=CC=CC=C4)C(NC(C)C)=O)=C1
Shipping

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

Ethanol : 51.864 mg/mL (100.00 mM; Need ultrasonic)

DMSO : 51.864 mg/mL (100.00 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 1.9281 mL 9.6406 mL 19.2812 mL
5 mM 0.3856 mL 1.9281 mL 3.8562 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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
Ethanol / DMSO 1 mM 1.9281 mL 9.6406 mL 19.2812 mL 48.2030 mL
5 mM 0.3856 mL 1.9281 mL 3.8562 mL 9.6406 mL
10 mM 0.1928 mL 0.9641 mL 1.9281 mL 4.8203 mL
15 mM 0.1285 mL 0.6427 mL 1.2854 mL 3.2135 mL
20 mM 0.0964 mL 0.4820 mL 0.9641 mL 2.4101 mL
25 mM 0.0771 mL 0.3856 mL 0.7712 mL 1.9281 mL
30 mM 0.0643 mL 0.3214 mL 0.6427 mL 1.6068 mL
40 mM 0.0482 mL 0.2410 mL 0.4820 mL 1.2051 mL
50 mM 0.0386 mL 0.1928 mL 0.3856 mL 0.9641 mL
60 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8034 mL
80 mM 0.0241 mL 0.1205 mL 0.2410 mL 0.6025 mL
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ACT-335827 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:

ACT-3358271354039-86-3ACT335827ACT 335827Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT Receptororexin receptor antagonistOXR1OXR2neurotransmitterneurological disordersInhibitorinhibitorinhibit

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