An orexin receptor 2 agonist
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TAK-994

Item No. 42336

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(2S,3S)-1-(2-hydroxy-2-methyl-1-oxopropyl)-2-[(2,3',5'-trifluoro[1,1'-biphenyl]-3-yl)methyl]-3-pyrrolidinyl]-methanesulfonamide
CAS Number
2274802-95-6
Synonyms
  • Firazorexton
Molecular Formula
C22H25F3N2O4S
Formula Weight
470.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mLDMSO: Sparingly Soluble: 1-10 mg/mL
SMILES
CC(C)(O)C(N(CC[C@@H]1NS(=O)(C)=O)[C@H]1CC2=C(C(C3=CC(F)=CC(F)=C3)=CC=C2)F)=O
InChi Code
InChI=1S/C22H25F3N2O4S/c1-22(2,29)21(28)27-8-7-18(26-32(3,30)31)19(27)11-13-5-4-6-17(20(13)25)14-9-15(23)12-16(24)10-14/h4-6,9-10,12,18-19,26,29H,7-8,11H2,1-3H3/t18-,19-/m0/s1
InChi Key
VOSAWOSMGPKQEQ-OALUTQOASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $435

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    5 mg

    $1,522

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    10 mg

    $2,173

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    Product Description

    TAK-994 is an orexin receptor 2 (OX2R) agonist.1,2 It selectively induces calcium mobilization in CHO-K1 cells expressing human OX2R over those expressing OX1R (EC50s = 0.019 and 14 µM, respectively).1 TAK-994 is also selective for OX2R over a panel of 106 enzymes, receptors, and ion channels at 10 µM. In vivo, TAK-994 (3 mg/kg) increases wakefulness time and wakefulness episode duration and inhibits chocolate-induced cataplexy-like episodes during the active phase in a model of narcolepsy using mice with orexin neurons ablated by ataxin-3 expression. It increases wakefulness time but does not affect orexin A (OXA) or OXB cerebrospinal fluid (CSF) levels during the sleep phase in cynomolgus monkeys when administered at a dose of 10 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ishikawa, T., Hara, H., Kawano, A., et al. TAK-994, a novel orally available brain-penetrant orexin 2 receptor-selective agonist, suppresses fragmentation of wakefulness and cataplexy-like episodes in mouse models of narcolepsy. J. Pharmacol. Exp. Ther. 385(3), 193-204 (2023).

    2. Yamada, R., Narita, N., Ishikawa, T., et al. The orexin receptor 2 (OX2R)-selective agonist TAK-994 increases wakefulness without affecting cerebrospinal fluid orexin levels in cynomolgus monkeys. Pharmacol. Biochem. Behav. 234, 173690 (2024).