ML204
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MedKoo CAT#: 522358

CAS#: 5465-86-1 (free base)

Description: ML204 is a novel and potential TRPC4 Channel inhibitor. ML204 inhibited TRPC4β-mediated intracellular Ca(2+) rise with an IC(50) value of 0.96 μm and exhibited 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation. ML204 represents an excellent novel tool for investigation of TRPC4 channel function and may facilitate the development of therapeutics targeted to TRPC4.


Chemical Structure

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ML204
CAS# 5465-86-1 (free base)

Theoretical Analysis

MedKoo Cat#: 522358
Name: ML204
CAS#: 5465-86-1 (free base)
Chemical Formula: C15H18N2
Exact Mass: 226.147
Molecular Weight: 226.32
Elemental Analysis: C, 79.61; H, 8.02; N, 12.38

Price and Availability

Size Price Availability Quantity
50.0mg USD 150.0 Same day
100.0mg USD 250.0 Same day
200.0mg USD 450.0 Same day
500.0mg USD 950.0 Same day
1.0g USD 1450.0 Same day
2.0g USD 2450.0 Same day
5.0g USD 3850.0 2 Weeks
10.0g USD 5950.0 2 Weeks
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Related CAS #: 5465-86-1 (free base)   2070015-10-8 (HCl)    

Synonym: ML204; ML-204; ML 204; ML204 free base

IUPAC/Chemical Name: 4-Methyl-2-(1-piperidinyl)quinoline

InChi Key: USYRQXDHKXGTCK-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H18N2/c1-12-11-15(17-9-5-2-6-10-17)16-14-8-4-3-7-13(12)14/h3-4,7-8,11H,2,5-6,9-10H2,1H3

SMILES Code: CC1=CC(N2CCCCC2)=NC3=CC=CC=C13

Appearance: Off-white 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, not in water

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

Preparing Stock Solutions

The following data is based on the product molecular weight 226.32 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

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1: Lindström JB, Pierce NT, Latz MI. Role of TRP Channels in Dinoflagellate Mechanotransduction. Biol Bull. 2017 Oct;233(2):151-167. doi: 10.1086/695421. Epub 2018 Jan 3. PubMed PMID: 29373067.

2: Wang X, Dande RR, Yu H, Samelko B, Miller RE, Altintas MM, Reiser J. TRPC5 Does Not Cause or Aggravate Glomerular Disease. J Am Soc Nephrol. 2018 Feb;29(2):409-415. doi: 10.1681/ASN.2017060682. Epub 2017 Oct 23. PubMed PMID: 29061651; PubMed Central PMCID: PMC5791075.

3: Maddox JW, Khorsandi N, Gleason E. TRPC5 is required for the NO-dependent increase in dendritic Ca(2+) and GABA release from chick retinal amacrine cells. J Neurophysiol. 2018 Jan 1;119(1):262-273. doi: 10.1152/jn.00500.2017. Epub 2017 Oct 4. PubMed PMID: 28978766.

4: Ilatovskaya DV, Palygin O, Levchenko V, Endres BT, Staruschenko A. The Role of Angiotensin II in Glomerular Volume Dynamics and Podocyte Calcium Handling. Sci Rep. 2017 Mar 22;7(1):299. doi: 10.1038/s41598-017-00406-2. PubMed PMID: 28331185; PubMed Central PMCID: PMC5428415.

5: Griffin CS, Bradley E, Dudem S, Hollywood MA, McHale NG, Thornbury KD, Sergeant GP. Muscarinic Receptor Induced Contractions of the Detrusor are Mediated by Activation of TRPC4 Channels. J Urol. 2016 Dec;196(6):1796-1808. doi: 10.1016/j.juro.2016.05.108. Epub 2016 Jun 7. PubMed PMID: 27287524.

6: Gómez M, González A, Sáez CA, Moenne A. Copper-Induced Membrane Depolarizations Involve the Induction of Mosaic TRP Channels, Which Activate VDCC Leading to Calcium Increases in Ulva compressa. Front Plant Sci. 2016 Jun 14;7:754. doi: 10.3389/fpls.2016.00754. eCollection 2016. PubMed PMID: 27379106; PubMed Central PMCID: PMC4905984.

7: Alawi KM, Russell FA, Aubdool AA, Srivastava S, Riffo-Vasquez Y, Baldissera L Jr, Thakore P, Saleque N, Fernandes ES, Walsh DA, Brain SD. Transient receptor potential canonical 5 (TRPC5) protects against pain and vascular inflammation in arthritis and joint inflammation. Ann Rheum Dis. 2017 Jan;76(1):252-260. doi: 10.1136/annrheumdis-2015-208886. Epub 2016 May 10. PubMed PMID: 27165180; PubMed Central PMCID: PMC5264234.

8: Zhang L, Kolaj M, Renaud LP. Endocannabinoid 2-AG and intracellular cannabinoid receptors modulate a low-threshold calcium spike-induced slow depolarizing afterpotential in rat thalamic paraventricular nucleus neurons. Neuroscience. 2016 May 13;322:308-19. doi: 10.1016/j.neuroscience.2016.02.047. Epub 2016 Feb 26. PubMed PMID: 26924019.

9: Carson C, Raman P, Tullai J, Xu L, Henault M, Thomas E, Yeola S, Lao J, McPate M, Verkuyl JM, Marsh G, Sarber J, Amaral A, Bailey S, Lubicka D, Pham H, Miranda N, Ding J, Tang HM, Ju H, Tranter P, Ji N, Krastel P, Jain RK, Schumacher AM, Loureiro JJ, George E, Berellini G, Ross NT, Bushell SM, Erdemli G, Solomon JM. Englerin A Agonizes the TRPC4/C5 Cation Channels to Inhibit Tumor Cell Line Proliferation. PLoS One. 2015 Jun 22;10(6):e0127498. doi: 10.1371/journal.pone.0127498. eCollection 2015. PubMed PMID: 26098886; PubMed Central PMCID: PMC4476799.

10: Zhao PY, Gan G, Peng S, Wang SB, Chen B, Adelman RA, Rizzolo LJ. TRP Channels Localize to Subdomains of the Apical Plasma Membrane in Human Fetal Retinal Pigment Epithelium. Invest Ophthalmol Vis Sci. 2015 Mar 3;56(3):1916-23. doi: 10.1167/iovs.14-15738. PubMed PMID: 25736794; PubMed Central PMCID: PMC4364639.

11: Antolín AA, Mestres J. Distant polypharmacology among MLP chemical probes. ACS Chem Biol. 2015 Feb 20;10(2):395-400. doi: 10.1021/cb500393m. Epub 2014 Nov 6. PubMed PMID: 25365788.

12: Kolaj M, Zhang L, Renaud LP. Novel coupling between TRPC-like and KNa channels modulates low threshold spike-induced afterpotentials in rat thalamic midline neurons. Neuropharmacology. 2014 Nov;86:88-96. doi: 10.1016/j.neuropharm.2014.06.023. Epub 2014 Jul 9. PubMed PMID: 25014020.

13: Freichel M, Tsvilovskyy V, Camacho-Londoño JE. TRPC4- and TRPC4-containing channels. Handb Exp Pharmacol. 2014;222:85-128. doi: 10.1007/978-3-642-54215-2_5. Review. PubMed PMID: 24756704.

14: Zhang L, Kolaj M, Renaud LP. GIRK-like and TRPC-like conductances mediate thyrotropin-releasing hormone-induced increases in excitability in thalamic paraventricular nucleus neurons. Neuropharmacology. 2013 Sep;72:106-15. doi: 10.1016/j.neuropharm.2013.04.023. Epub 2013 Apr 28. PubMed PMID: 23632082.

15: Miller MR, Shi J, Wu M, Engers J, Hopkins CR, Lindsley CW, Salovich JM, Zhu Y, Tian JB, Zhu MX, McManus OB, Li M. Novel Chemical Inhibitor of TRPC4 Channels. 2010 Dec 15 [updated 2011 May 26]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. Available from http://www.ncbi.nlm.nih.gov/books/NBK65430/ PubMed PMID: 22049577.

16: Miller M, Shi J, Zhu Y, Kustov M, Tian JB, Stevens A, Wu M, Xu J, Long S, Yang P, Zholos AV, Salovich JM, Weaver CD, Hopkins CR, Lindsley CW, McManus O, Li M, Zhu MX. Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. J Biol Chem. 2011 Sep 23;286(38):33436-46. doi: 10.1074/jbc.M111.274167. Epub 2011 Jul 27. PubMed PMID: 21795696; PubMed Central PMCID: PMC3190871.

ML204

50.0mg / USD 150.0