RX821002 HCl
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Hodoodo CAT#: H532602

CAS#: 109544-45-8 (HCl)

Description: RX821002 is a potent, selective α2-adrenoceptor antagonist with very low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).


Chemical Structure

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RX821002 HCl
CAS# 109544-45-8 (HCl)

Theoretical Analysis

Hodoodo Cat#: H532602
Name: RX821002 HCl
CAS#: 109544-45-8 (HCl)
Chemical Formula: C12H15ClN2O3
Exact Mass: 0.00
Molecular Weight: 270.710
Elemental Analysis: C, 53.24; H, 5.59; Cl, 13.10; N, 10.35; O, 17.73

Price and Availability

Size Price Availability Quantity
10mg USD -2 2 Weeks
25mg USD -2 2 Weeks
5g USD -2 2 Weeks
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
500mg USD 1450 2 Weeks
1g USD 2250 2 Weeks
2g USD 3850 2 Weeks
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Related CAS #: 109544-45-8 (HCl)   102575-24-6 (free base)    

Synonym: RX821002; RX 821002; RX-821002; RX821002 HCl; RX821002 hydrochloride;

IUPAC/Chemical Name: 2-(2,3-Dihydro-2-methoxy-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole hydrochloride

InChi Key: IMPOOMVZVWKSAP-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H14N2O3.ClH/c1-15-12(11-13-6-7-14-11)8-16-9-4-2-3-5-10(9)17-12;/h2-5H,6-8H2,1H3,(H,13,14);1H

SMILES Code: COC1(C2=NCCN2)OC3=CC=CC=C3OC1.[H]Cl

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 270.71 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Sandner G, Angst MJ, Guiberteau T, Guignard B, Nehlig A. Effects of caffeine or RX821002 in rats with a neonatal ventral hippocampal lesion. Front Behav Neurosci. 2014 Jan 28;8:15. doi: 10.3389/fnbeh.2014.00015. PMID: 24478661; PMCID: PMC3904090.


2: Holmberg M, Fagerholm V, Scheinin M. Regional distribution of alpha(2C)-adrenoceptors in brain and spinal cord of control mice and transgenic mice overexpressing the alpha(2C)-subtype: an autoradiographic study with [(3)H]RX821002 and [(3)H]rauwolscine. Neuroscience. 2003;117(4):875-98. doi: 10.1016/s0306-4522(02)00966-1. PMID: 12654340.


3: Uhlén S, Dambrova M, Näsman J, Schiöth HB, Gu Y, Wikberg-Matsson A, Wikberg JE. [3H]RS79948-197 binding to human, rat, guinea pig and pig alpha2A-, alpha2B- and alpha2C-adrenoceptors. Comparison with MK912, RX821002, rauwolscine and yohimbine. Eur J Pharmacol. 1998 Feb 5;343(1):93-101. doi: 10.1016/s0014-2999(97)01521-5. PMID: 9551719.


4: Callado LF, Meana JJ. Low-affinity conditions for agonists increase the binding of the antagonist [3H]RX821002 to the alpha(2B/C)-adrenoceptor subtypes in human brain and rat kidney. Eur J Pharmacol. 1997 Jul 30;332(1):109-12. doi: 10.1016/s0014-2999(97)01105-9. PMID: 9298931.


5: Chan SL, Scarpello KE, Morgan NG. Identification and characterization of non- adrenergic binding sites in insulin-secreting cells with the imidazoline RX821002. Adv Exp Med Biol. 1997;426:159-63. doi: 10.1007/978-1-4899-1819-2_21. PMID: 9544269.


6: Callado LF, Gabilondo AM, Meana JJ. [3H]RX821002 (2-methoxyidazoxan) binds to alpha 2-adrenoceptor subtypes and a non-adrenoceptor imidazoline binding site in rat kidney. Eur J Pharmacol. 1996 Dec 5;316(2-3):359-68. doi: 10.1016/s0014-2999(96)00692-9. PMID: 8982708.


7: Deupree JD, Hinton KA, Cerutis DR, Bylund DB. Buffers differentially alter the binding of [3H]rauwolscine and [3H]RX821002 to the alpha-2 adrenergic receptor subtypes. J Pharmacol Exp Ther. 1996 Sep;278(3):1215-27. PMID: 8819505.


8: Grijalba B, Callado LF, Javier Meana J, García-Sevilla JA, Pazos A. Alpha 2-adrenoceptor subtypes in the human brain: a pharmacological delineation of [3H]RX-821002 binding to membranes and tissue sections. Eur J Pharmacol. 1996 Aug 22;310(1):83-93. doi: 10.1016/0014-2999(96)00381-0. PMID: 8880071.


9: Halme M, Sjöholm B, Savola JM, Scheinin M. Recombinant human alpha 2-adrenoceptor subtypes: comparison of [3H]rauwolscine, [3H]atipamezole and [3H]RX821002 as radioligands. Biochim Biophys Acta. 1995 Apr 28;1266(2):207-14. doi: 10.1016/0167-4889(95)90410-i. PMID: 7742388.


10: Renouard A, Widdowson PS, Millan MJ. Multiple alpha 2 adrenergic receptor subtypes. I. Comparison of [3H]RX821002-labeled rat R alpha-2A adrenergic receptors in cerebral cortex to human H alpha2A adrenergic receptor and other populations of alpha-2 adrenergic subtypes. J Pharmacol Exp Ther. 1994 Sep;270(3):946-57. PMID: 7932207.


11: Sastre M, García-Sevilla JA. Alpha 2-adrenoceptor subtypes identified by [3H]RX821002 binding in the human brain: the agonist guanoxabenz does not discriminate different forms of the predominant alpha 2A subtype. J Neurochem. 1994 Sep;63(3):1077-85. doi: 10.1046/j.1471-4159.1994.63031077.x. PMID: 7914222.


12: Wallace DR, Muskardin DT, Zahniser NR. Pharmacological characterization of [3H]idazoxan, [3H]RX821002 and p-[125I]iodoclonidine binding to alpha 2-adrenoceptors in rat cerebral cortical membranes. Eur J Pharmacol. 1994 Jun 2;258(1-2):67-76. doi: 10.1016/0014-2999(94)90058-2. PMID: 7925601.


13: O'Rourke MF, Blaxall HS, Iversen LJ, Bylund DB. Characterization of [3H]RX821002 binding to alpha-2 adrenergic receptor subtypes. J Pharmacol Exp Ther. 1994 Mar;268(3):1362-7. PMID: 7908054.


14: Devedjian JC, Esclapez F, Denis-Pouxviel C, Paris H. Further characterization of human alpha 2-adrenoceptor subtypes: [3H]RX821002 binding and definition of additional selective drugs. Eur J Pharmacol. 1994 Jan 24;252(1):43-9. doi: 10.1016/0014-2999(94)90573-8. PMID: 7908642.


15: Miralles A, Olmos G, Sastre M, Barturen F, Martin I, Garcia-Sevilla JA. Discrimination and pharmacological characterization of I2-imidazoline sites with [3H]idazoxan and alpha-2 adrenoceptors with [3H]RX821002 (2-methoxy idazoxan) in the human and rat brains. J Pharmacol Exp Ther. 1993 Mar;264(3):1187-97. PMID: 8095548.


16: Uhlén S, Wikberg JE. Rat spinal cord alpha 2-adrenoceptors are of the alpha 2A-subtype: comparison with alpha 2A- and alpha 2B-adrenoceptors in rat spleen, cerebral cortex and kidney using 3H-RX821002 ligand binding. Pharmacol Toxicol. 1991 Nov;69(5):341-50. doi: 10.1111/j.1600-0773.1991.tb01308.x. PMID: 1687079.


17: Uhlén S, Wikberg JE. Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound. Eur J Pharmacol. 1991 Sep 17;202(2):235-43. doi: 10.1016/0014-2999(91)90299-6. PMID: 1666366.


18: Paris H, Voisin T, Remaury A, Rouyer-Fessard C, Daviaud D, Langin D, Laburthe M. Alpha-2 adrenoceptor in rat jejunum epithelial cells: characterization with [3H]RX821002 and distribution along the villus-crypt axis. J Pharmacol Exp Ther. 1990 Sep;254(3):888-93. PMID: 1975626.


19: Galitzky J, Senard JM, Lafontan M, Stillings M, Montastruc JL, Berlan M. Identification of human platelet alpha 2-adrenoceptors with a new antagonist [3H]-RX821002, a 2-methoxy derivative of idazoxan. Br J Pharmacol. 1990 Aug;100(4):862-6. doi: 10.1111/j.1476-5381.1990.tb14105.x. PMID: 1976403; PMCID: PMC1917581.


20: Langin D, Paris H, Lafontan M. Binding of [3H]idazoxan and of its methoxy derivative [3H] RX821002 in human fat cells: [3H]idazoxan but not [3H] RX821002 labels additional non-alpha 2-adrenergic binding sites. Mol Pharmacol. 1990 Jun;37(6):876-85. PMID: 1972775.