TCS-OX2-29 free base

MedKoo Cat#: 555916 | Name: TCS-OX2-29 free base

Description:

WARNING: This product is for research use only, not for human or veterinary use.

TCS-OX2-29 is a selective OX2 receptor antagonist (IC50 = 40 nM). Orexin, which is mainly produced by orexin-expressing neurons in the lateral hypothalamus (LH), plays an important role in pain modulation. Both kinds of orexin-1 (Ox1) and orexin-2 (Ox2) receptors have been found at high density in the ventral tegmental area (VTA) and nucleus accumbens (NAc).

Chemical Structure

TCS-OX2-29 free base

CAS#372523-75-6 (free base)

Theoretical Analysis

MedKoo Cat#: 555916

Name: TCS-OX2-29 free base

CAS#: 372523-75-6 (free base)

Chemical Formula: C23H31N3O3

Exact Mass: 397.2365

Molecular Weight: 397.52

Elemental Analysis: C, 69.49; H, 7.86; N, 10.57; O, 12.07

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 1,850.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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Related CAS #

1610882-30-8 (HCl) 372523-75-6 (free base)

Synonym

TCS-OX2-29 free base; TCS-OX2-29; TCS-OX229; TCS-OX2 29; TCS-OX 229; TCS-OX 229; TCSOX229; TCSOX-229; TCSOX 229;

IUPAC/Chemical Name

(2S)-1-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone

InChi Key

COFVZFLCAOUMJT-OAQYLSRUSA-N

InChi Code

InChI=1S/C23H31N3O3/c1-23(2,3)21(25-14-16-6-9-24-10-7-16)22(27)26-11-8-17-12-19(28-4)20(29-5)13-18(17)15-26/h6-7,9-10,12-13,21,25H,8,11,14-15H2,1-5H3/t21-/m1/s1

SMILES Code

CC(C)(C)[C@H](NCC1=CC=NC=C1)C(N2CC3=C(C=C(OC)C(OC)=C3)CC2)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

	Solvent	mg/mL	mM
Solubility
	Soluble in DMSO	0.0	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 397.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Chen YT, Young TH, Wang YH, Huang CH, Gao YY, Huang TW. Orexin-A increases the differentiation of human olfactory sensory neurons through orexin receptor type 1. Regen Ther. 2024 Nov 8;26:1058-1068. doi: 10.1016/j.reth.2024.10.014. PMID: 39582799; PMCID: PMC11585478. 2: Anna S, Jan W, Aleksandra S, Piotr D, Tomasz K, Artur W, Iwona B, Ewa P, Ewa RW, Paweł D, Laretta GD, Joanna KB, Gieleta AW, Paweł B, Artur J, Marcin M, Andrzej W. The Orexin OX2 Receptor-Dependent Pathway Is Implicated in the Development of Overactive Bladder and Depression in Rats Exposed to Corticosterone. Neurourol Urodyn. 2024 Oct 14. doi: 10.1002/nau.25602. Epub ahead of print. PMID: 39402852. 3: Danesh E, Hassanpour S, Vazir B, Saghafi M, Ghalandari-Shamami M, Haghparast A. The restraint stress-induced antinociceptive effects decreased by antagonism of both orexin receptors within the CA1 region of the hippocampus. Neuropeptides. 2024 Oct;107:102463. doi: 10.1016/j.npep.2024.102463. Epub 2024 Aug 22. PMID: 39180799. 4: Farmani D, Moteshakereh SM, Nikoohemmat M, Askari R, Salehi S, Haghparast A. Restraint stress-induced antinociceptive effects in acute pain: Involvement of orexinergic system in the nucleus accumbens. Behav Brain Res. 2024 Aug 24;472:115133. doi: 10.1016/j.bbr.2024.115133. Epub 2024 Jul 1. PMID: 38960330. 5: Yamada R, Koike T, Nakakariya M, Kimura H. Orexin receptor 2 agonist activates diaphragm and genioglossus muscle through stimulating inspiratory neurons in the pre-Bötzinger complex, and phrenic and hypoglossal motoneurons in rodents. PLoS One. 2024 Jun 25;19(6):e0306099. doi: 10.1371/journal.pone.0306099. PMID: 38917189; PMCID: PMC11198781. 6: Haddad M, Khazali H, Janahmadi M, Ghanbarian H. The differential effects of blocking retinal orexin receptors on the expression of retinal c-fos and hypothalamic Vip, PACAP, Bmal1, and c-fos in Male Wistar Rats. Exp Eye Res. 2024 Jul;244:109943. doi: 10.1016/j.exer.2024.109943. Epub 2024 May 24. PMID: 38797259. 7: Moshrefi F, Farrokhi AM, Fattahi M, Azizbeigi R, Haghparast A. The role of orexin receptors within the CA1 area in the acquisition and expression of methamphetamine place preference. J Psychiatr Res. 2024 Apr;172:291-299. doi: 10.1016/j.jpsychires.2024.02.051. Epub 2024 Feb 26. PMID: 38428165. 8: Fartootzadeh R, Taheri RA, Nourani MR, Goudarzi K. Orexin and cannabinoid systems modulate long-term potentiation of the hippocampus CA1 area in anesthetized rats. Iran J Basic Med Sci. 2024;27(4):461-465. doi: 10.22038/IJBMS.2023.73979.16075. PMID: 38419882; PMCID: PMC10897562. 9: Zokaei L, Akbari E, Babapour V, Zendehdel M. The Modulatory Role of Orexin 1 Receptor in Nucleus Accumbens (NAc) on Spatial Memory in Rats. Arch Razi Inst. 2023 Aug 31;78(4):1285-1294. doi: 10.32592/ARI.2023.78.4.1285. PMID: 38226387; PMCID: PMC10787936. 10: Pan L, Xiao S, Xu Z, Li W, Zhao L, Zhang L, Qi R, Wang J, Cai Y. Orexin-A attenuated motion sickness through modulating neural activity in hypothalamus nuclei. Br J Pharmacol. 2024 May;181(9):1474-1493. doi: 10.1111/bph.16307. Epub 2024 Jan 25. PMID: 38129941. 11: Nikoohemmat M, Farmani D, Moteshakereh SM, Salehi S, Rezaee L, Haghparast A. Intra-accumbal orexinergic system contributes to the stress-induced antinociceptive behaviors in the animal model of acute pain in rats. Behav Pharmacol. 2024 Apr 1;35(2-3):92-102. doi: 10.1097/FBP.0000000000000763. Epub 2024 Feb 23. PMID: 38055726. 12: Baghani M, Bolouri-Roudsari A, Askari R, Haghparast A. Orexin receptors in the hippocampal dentate gyrus modulated the restraint stress-induced analgesia in the animal model of chronic pain. Behav Brain Res. 2024 Feb 29;459:114772. doi: 10.1016/j.bbr.2023.114772. Epub 2023 Nov 22. PMID: 37995966. 13: Sadeghi M, Zareie F, Gholami M, Nazari-Serenjeh F, Ghalandari-Shamami M, Haghparast A. Contribution of the intra-hippocampal orexin system in the regulation of restraint stress response to pain-related behaviors in the formalin test. Behav Pharmacol. 2024 Apr 1;35(2-3):103-113. doi: 10.1097/FBP.0000000000000755. Epub 2023 Nov 7. PMID: 37934654. 14: Zamanirad F, Eskandari K, Mousavi Z, Haghparast A. Blockade of the orexin-2 receptors within the ventral tegmental area facilitates the extinction and prevents the reinstatement of methamphetamine-seeking behavior. Physiol Behav. 2024 Jan 1;273:114382. doi: 10.1016/j.physbeh.2023.114382. Epub 2023 Oct 20. PMID: 37866644. 15: Bolouri-Roudsari A, Baghani M, Askari K, Mazaheri S, Haghparast A. The integrative role of orexin-1 and orexin-2 receptors within the hippocampal dentate gyrus in the modulation of the stress-induced antinociception in the formalin pain test in the rat. Behav Pharmacol. 2024 Feb 1;35(1):14-25. doi: 10.1097/FBP.0000000000000737. Epub 2023 Aug 15. PMID: 37578388. 16: Panahi PS, Esmaili S, Ghalandari-Shamami M, Mousavi Z, Haghparast A. Similar functional roles of the Orexin-1 and Orexin-2 receptors within the dentate gyrus area of the hippocampus in the stress-induced antinociceptive responses in the acute pain model in the rat. Physiol Behav. 2023 Oct 15;270:114311. doi: 10.1016/j.physbeh.2023.114311. Epub 2023 Aug 1. PMID: 37536620. 17: Mazaheri S, Zendehdel M, Haghparast A. Restraint stress potentiates sensitivity to the antinociceptive effect of morphine through orexin receptors in the ventral tegmental area. Neuropeptides. 2023 Oct;101:102353. doi: 10.1016/j.npep.2023.102353. Epub 2023 Jun 15. PMID: 37385145. 18: Modaberi S, Amirteymori H, Mesgar S, Eskandari K, Haghparast A. The blockade of orexin receptors within the dentate gyrus of the hippocampus attenuated methamphetamine-induced reward learning during conditioning place preference. Pharmacol Biochem Behav. 2023 May;226:173559. doi: 10.1016/j.pbb.2023.173559. Epub 2023 Apr 24. PMID: 37100179. 19: Luan JC, Zhang QJ, Zhou X, Zhou X, Gu Q, Xia JD, Song NH. Orexin receptors in paraventricular nucleus influence sexual behavior via regulating the sympathetic outflow in males. Andrology. 2024 Jan;12(1):198-210. doi: 10.1111/andr.13444. Epub 2023 May 4. PMID: 37084406. 20: Moteshakereh SM, Nikoohemmat M, Farmani D, Khosrowabadi E, Salehi S, Haghparast A. The stress-induced antinociceptive responses to the persistent inflammatory pain involve the orexin receptors in the nucleus accumbens. Neuropeptides. 2023 Apr;98:102323. doi: 10.1016/j.npep.2023.102323. Epub 2023 Jan 28. PMID: 36736068.