Wako Pure Chemical Industries, Ltd.Wako Pure Chemical Industries, Ltd. - Laboratory Chemicals

For research on sleep/food intake
Orexins

Orexins are neuropeptides produced by some neurons in the lateral hypothalamic area. There are two types of orexins: Orexin-A and -B. Both are endogenous agonists against orexin receptors. There are two subtypes of orexin receptor: Orexin-1 receptor (OX1R) and -2 receptor (OX2R).   OX1R shows about 50 times higher affinity for orexin-A in comparison with the one for orexin-B. OX2R has similar affinity for both orexin A and orexin B.
As a pharmacological action of orexin, its involvement with sleep/waking and feeding behavior has been reported. Recently it has been cleared that it is deeply involved with the pathology of narcolepsy, which is one of the sleep disorders, and much attention has been attracted in sleep disorders research.


1. Orexins



Orexin A (Human)

  • Assay (HPLC): 95.0+ %
  • Solubility: Soluble in water.
  • CAS No.205640-90-0
  • C152 H243 N47 O44 S4 = 3561.10

Wako Catalog No. 159-03161 (0.1 mg)

Pyr-Pro-Leu-Pro-Asp-Cys-Cys-Arg-Gln-Lys-Thr-Cys-Ser-Cys-
Arg-Leu-Tyr-Glu-Leu-Leu-His-Gly-Ala-Gly-Asn-His-Ala-Ala-
Gly-Ile-Leu-Thr-Leu-NH2
(Disulfide bonds between Cys6-Cys12 and Cys7-Cys14)

Orexin B (Human)

  • Assay (HPLC): 95.0+ %
  • Solubility: Soluble in water.
  • CAS No.205640-91-1
  • C123 H212 N44 O35 S = 2899.34

Wako Catalog No. 156-03171 (0.1 mg)

Arg-Ser-Gly-Pro-Pro-Gly-Leu-Gln-Gly-Arg-Leu-Gln-Arg-Leu-
Leu-Gln-Ala-Ser-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2


Orexin B (Rat, Mouse)

  • Assay (HPLC): 95.0+ %
  • Solubility: Soluble in water.
  • CAS No.202801-92-1
  • C126 H215 N45 O34 S = 2936.40

Wako Catalog No. 153-03181 (0.1 mg)

Arg-Pro-Gly-Pro-Pro-Gly-Leu-Gln-Gly-Arg-Leu-Gln-Arg-Leu-
Leu-Gln-Ala-Asn-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2



2. Orexin Receptor Agonists


[Ala11, D-Leu]-Orexin B

This product is a selective agonist of orexin 2 receptor (OX2R). It is about 400 times more selective for OX2R compared to OX1R. 1)
  • Assay (HPLC): 90.0+ %
  • Solubility: Soluble in water.
  • CAS No.532932-99-3
  • C120H206N44O35S = 2857.26
  • EC50=0.13 nmol/L (OX2R), 52 nmol/L (OX1R) 1)
Wako Catalog No. 159-03161 (1 mg)

H-Arg-Ser-Gly-Pro-Pro-Gly-Leu-Gln-Gly-Arg-Ala-Gln-Arg-Leu-
D-Leu-Gln-Ala-Ser-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2

SB-668875

SB-668875 is a selective peptide agonist of orexin 2 receptor (OX2R).
  • Assay (HPLC): 99.46%
    (actual measured value of first lot)
  • Solubility: Soluble in water.
  • CAS No. 274252-40-3
  • C120H206N44O35S = 2857.26
Wako Catalog No. 194-17221 (1 mg)

H-Arg-Ser-Gly-Pro-Pro-Gly-Leu-Gln-Gly-Arg-Ala-Gln-Arg-Leu-
Leu-Gln-Ala-Ser-Gly-Asn-His-Ala-Ala-Gly-Ile-Leu-Thr-Met-NH2

YNT-185·2HCl

⇒ homepage
YNT-185·2HCl is non-peptide orexin 2 receptor (OX2R) agonist.
  • Assay (HPLC): 98.0+ %
  • Solubility: Saline (pH 2.4*) ··· 1.3 mol/L
  • CAS No. 1804978-82-2 (anhydride)
  • C33H37N5O5S·2HCl·nH2O (C33H37N5O5S·2HCl = 688.66)
Wako Catalog No. 254-00641 (5 mg); 254-00643 (100 mg)


3. Orexin Receptor Antagonists


JNJ 10397049

Potent selective OX2 receptor (OX2R) antagonist. Achieve more than 600 times the selectivity of OX1R 2).
Shows high level of OX2 receptor occupancy in the rat brain and exhibits sleep promoting effects.
  • Assay (HPLC): 98.0+ %
  • Solubility: Soluble in acetonitrile
  • CAS No. 708275-58-5
  • C19H20Br2N2O3 = 484.18
  • pKi=8.3 (OX2R), 5.5(OX1R) 2)
Wako Catalog No. 104-00171 (10 mg); 100-00173 (50 mg); 108-00174 (250 mg)

JNJ 10397049

SB-408124

Selective non-peptide orexin 1 receptor (OX1R) antagonist
  • Assay (HPLC): 98.0+ %
  • Solubility: Soluble in DMSO.
  • CAS No. 288150-92-5
  • C19H18F2N4O=356.37
  • Kb=21.7 nmol/L (OX1R), 1,405 nmol/L (OX2R) 3)
Wako Catalog No. 196-17421 (5 mg); 192-17423 (25 mg)

SB-408124

SB-674042

Selective non-peptide orexin 1 receptor (OX1R) antagonist
  • Assay (HPLC): 98.0+ %
  • Solubility: Soluble in DMSO.
  • CAS No. 483313-22-0
  • C24H21FN4O2S=448.51
  • Kb=1.1 nmol/L (OX1R), 129 nmol/L (OX2R) 3)
Wako Catalog No. 192-17761 (5 mg); 198-17763 (25 mg)

SB-674042

4. References



  1. Sakane, F., Imai, S., Kai, M., Wada, I. and Kanoh, H. : J. Biol. Chem., 271, 8394 (1996)
  2. McAtee, L. C., Sutton, S. W., Rudolph, D. A., Li, X., Aluisio, L. E., Phuong, V. K., Dvorak, C. A., Lovenberg, T. W., Carruthers, N. I. and Jones, T. K. : Bioorg. Med. Chem. Lett., 14, 4225(2004).
  3. Imai, S., Yasuda, S., Kai, M., Kanoh, H. and Sakane, F. : Biochim. Biophys. Acta, 1791, 246 (2009)

5. Product List


Product Name Package Size Wako Cat. No. Storage Condition Grade
Orexins
Orexin A(Human)
0.1 mg
Keep at -20°C
for Cellbiology
Orexin B(Human)
0.1 mg
Orexin B(Rat, Mouse)
0.1 mg
Orexin Receptor Agonists
[Ala11, D-Leu15]-Orexin B
1 mg
Keep at -20°C.
for Cellbiology
SB-668875
1 mg
YNT-185·2HCl
5 mg
100 mg
Orexin Receptor Antagonists
JNJ 10397049
10 mg
Keep at 2-10°C.
for Cellbiology
50 mg
250 mg
SB-408124
5 mg
Keep at -20°C.
25 mg
SB-674042
5 mg
25 mg