KF 17837S | CAS#152881-18-0 | A(2a) receptor antagonist |MedKoo

MedKoo Cat#: 531999 | Name: KF 17837S

Description:

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

KF 17837S is an adenosine A(2a) receptor antagonists, which is potential therapeutic and neuroprotective effects in Parkinson's disease.

Chemical Structure

KF 17837S

CAS#152881-18-0

Theoretical Analysis

MedKoo Cat#: 531999

Name: KF 17837S

CAS#: 152881-18-0

Chemical Formula: C20H26N4O4

Exact Mass: 386.1954

Molecular Weight: 386.45

Elemental Analysis: C, 62.16; H, 6.78; N, 14.50; O, 16.56

Price and Availability

Size	Price	Availability
50mg	USD 2,750.00	2 Weeks
100mg	USD 3,650.00	2 Weeks
200mg	USD 5,450.00	2 Weeks

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Synonym

KF 17837S; KF17837S; KF-17837S.

IUPAC/Chemical Name

8-(3,4-dimethoxyphenyl)-7-methyl-1,3-dipropylpurine-2,6-dione

InChi Key

FSUNYKAEJIVAHY-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H26N4O4/c1-6-10-23-18-16(19(25)24(11-7-2)20(23)26)22(3)17(21-18)13-8-9-14(27-4)15(12-13)28-5/h8-9,12H,6-7,10-11H2,1-5H3

SMILES Code

O=C(N1CCC)N(CCC)C2=C(N(C)C(C3=CC=C(OC)C(OC)=C3)=N2)C1=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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

KF 17837S is an adenosine A(2a) receptor antagonists.

In vitro activity:

The novel A2A receptor antagonist, (E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine (KF 17837), blocked the CGS 21680 (1 nM)-induced inhibition of [3H]-GABA efflux with an EC50 of approximately 30 nM and also antagonized the CGS 21680 (0.1 nM)-induced stimulation of [3H]-ACh release with an EC50 of approximately 0.3 nM. Reference: Br J Pharmacol. 1994 Sep;113(1):43-8. https://pubmed.ncbi.nlm.nih.gov/7812630/

In vivo activity:

Autoradiographic study of [3H]KF17837S binding using rat brain sections revealed that the binding site was highly enriched in the striatal region. These data indicate that [3H] KF17837S labels the adenosine A2A receptor in rat brain. Reference: Mol Pharmacol. 1994 Nov;46(5):817-22. https://pubmed.ncbi.nlm.nih.gov/7969067/

Preparing Stock Solutions

The following data is based on the product molecular weight 386.45 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

Formulation protocol:

1. Kurokawa M, Kirk IP, Kirkpatrick KA, Kase H, Richardson PJ. Inhibition by KF17837 of adenosine A2A receptor-mediated modulation of striatal GABA and ACh release. Br J Pharmacol. 1994 Sep;113(1):43-8. doi: 10.1111/j.1476-5381.1994.tb16171.x. PMID: 7812630; PMCID: PMC1510043. 2. Nonaka H, Ichimura M, Takeda M, Nonaka Y, Shimada J, Suzuki F, Yamaguchi K, Kase H. KF17837 ((E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine), a potent and selective adenosine A2 receptor antagonist. Eur J Pharmacol. 1994 May 17;267(3):335-41. doi: 10.1016/0922-4106(94)90159-7. PMID: 8088373. 3. Correa M, Wisniecki A, Betz A, Dobson DR, O'Neill MF, O'Neill MJ, Salamone JD. The adenosine A2A antagonist KF17837 reverses the locomotor suppression and tremulous jaw movements induced by haloperidol in rats: possible relevance to parkinsonism. Behav Brain Res. 2004 Jan 5;148(1-2):47-54. doi: 10.1016/s0166-4328(03)00178-5. PMID: 14684247. 4. Nonaka H, Mori A, Ichimura M, Shindou T, Yanagawa K, Shimada J, Kase H. Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes. Mol Pharmacol. 1994 Nov;46(5):817-22. PMID: 7969067.

In vitro protocol:

In vivo protocol:

1. Correa M, Wisniecki A, Betz A, Dobson DR, O'Neill MF, O'Neill MJ, Salamone JD. The adenosine A2A antagonist KF17837 reverses the locomotor suppression and tremulous jaw movements induced by haloperidol in rats: possible relevance to parkinsonism. Behav Brain Res. 2004 Jan 5;148(1-2):47-54. doi: 10.1016/s0166-4328(03)00178-5. PMID: 14684247. 2. Nonaka H, Mori A, Ichimura M, Shindou T, Yanagawa K, Shimada J, Kase H. Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes. Mol Pharmacol. 1994 Nov;46(5):817-22. PMID: 7969067.

1: Morelli M, Wardas J. Adenosine A(2a) receptor antagonists: potential therapeutic and neuroprotective effects in Parkinson's disease. Neurotox Res. 2001 Nov;3(6):545-56. PubMed PMID: 15111244. 2: Correa M, Wisniecki A, Betz A, Dobson DR, O'Neill MF, O'Neill MJ, Salamone JD. The adenosine A2A antagonist KF17837 reverses the locomotor suppression and tremulous jaw movements induced by haloperidol in rats: possible relevance to parkinsonism. Behav Brain Res. 2004 Jan 5;148(1-2):47-54. PubMed PMID: 14684247. 3: Bivalacqua TJ, Champion HC, Lambert DG, Kadowitz PJ. Vasodilator responses to adenosine and hyperemia are mediated by A(1) and A(2) receptors in the cat vascular bed. Am J Physiol Regul Integr Comp Physiol. 2002 Jun;282(6):R1696-709. PubMed PMID: 12010752.