AC1903 | CAS#831234-13-0 | TRPC5 channel blocker

AC1903
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561805

CAS#: 831234-13-0

Description: AC1903 is a specific blocker of TRPC5 channel activity. It has been shown to suppress severe proteinuria and prevent podocyte loss. AC1903 consistently suppressed G418 uptake and G418-induced PTC readthrough in the DMS-114 cancer cell line and junctional epidermolysis bullosa (JEB) patient-derived keratinocytes and inhibited TRPV4 channels, but had weak or no effects on TRPV1 and no effect on the nonselective cation channel PIEZO1

Chemical Structure

AC1903

CAS# 831234-13-0

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 561805
Name: AC1903
CAS#: 831234-13-0
Chemical Formula: C19H17N3O
Exact Mass: 303.14
Molecular Weight: 303.360
Elemental Analysis: C, 75.23; H, 5.65; N, 13.85; O, 5.27

Price and Availability

Size	Price	Availability
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3850	2 Weeks
2g	USD 6450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: AC1903; AC-1903; AC 1903;

IUPAC/Chemical Name: 1-Benzyl-N-(2-furylmethyl)-1H-benzimidazol-2-amine

InChi Key: OECUWHDVQIITIS-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H17N3O/c1-2-7-15(8-3-1)14-22-18-11-5-4-10-17(18)21-19(22)20-13-16-9-6-12-23-16/h1-12H,13-14H2,(H,20,21)

SMILES Code: C1(NCC2=CC=CO2)=NC3=CC=CC=C3N1CC4=CC=CC=C4

Appearance: Solid powder

Purity: >95% (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:

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Biological target:	AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties.
In vitro activity:	TBD
In vivo activity:	Twice-daily intraperitoneal injections of AC1903 (50 mg/kg) for 7 days suppressed severe proteinuria in AT1R Tg rats (Advanced) (Fig. 3A), without evidence of toxicity (fig. S7, A to C). Inside-out electrophysiology measurements in isolated glomeruli from AT1R Tg rats confirmed that AC1903 blocks TRPC5 channel activity during proteinuric disease progression (Fig. 3, B and C). Morphometric analysis demonstrated that treatment with AC1903 led to a significant reduction in pseudocyst formation and in podocyte loss in AT1R Tg rats with advanced disease (Fig. 3, D to F). Thus, AC1903 inhibits the progression of proteinuric kidney disease by preserving podocytes. Reference: Science. 2017 Dec 8; 358(6368): 1332–1336. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6014699/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	51.3	169.07
	DMSO:PBS (pH 7.2) (1:4)	0.2	0.66
	DMF	30.0	98.89
	Ethanol	30.5	100.54

Preparing Stock Solutions

The following data is based on the product molecular weight 303.36 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. Sharma SH, Pablo JL, Montesinos MS, Greka A, Hopkins CR. Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903. Bioorg Med Chem Lett. 2019 Jan 15;29(2):155-159. doi: 10.1016/j.bmcl.2018.12.007. Epub 2018 Dec 4. PMID: 30538066; PMCID: PMC6349029. 2. Zhou Y, Castonguay P, Sidhom EH, Clark AR, Dvela-Levitt M, Kim S, Sieber J, Wieder N, Jung JY, Andreeva S, Reichardt J, Dubois F, Hoffmann SC, Basgen JM, Montesinos MS, Weins A, Johnson AC, Lander ES, Garrett MR, Hopkins CR, Greka A. A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models. Science. 2017 Dec 8;358(6368):1332-1336. doi: 10.1126/science.aal4178. PMID: 29217578; PMCID: PMC6014699.
In vitro protocol:	TBD
In vivo protocol:	1. Sharma SH, Pablo JL, Montesinos MS, Greka A, Hopkins CR. Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903. Bioorg Med Chem Lett. 2019 Jan 15;29(2):155-159. doi: 10.1016/j.bmcl.2018.12.007. Epub 2018 Dec 4. PMID: 30538066; PMCID: PMC6349029. 2. Zhou Y, Castonguay P, Sidhom EH, Clark AR, Dvela-Levitt M, Kim S, Sieber J, Wieder N, Jung JY, Andreeva S, Reichardt J, Dubois F, Hoffmann SC, Basgen JM, Montesinos MS, Weins A, Johnson AC, Lander ES, Garrett MR, Hopkins CR, Greka A. A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models. Science. 2017 Dec 8;358(6368):1332-1336. doi: 10.1126/science.aal4178. PMID: 29217578; PMCID: PMC6014699.

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1: Zhou Y, Castonguay P, Sidhom EH, Clark AR, Dvela-Levitt M, Kim S, Sieber J, Wieder N, Jung JY, Andreeva S, Reichardt J, Dubois F, Hoffmann SC, Basgen JM, Montesinos MS, Weins A, Johnson AC, Lander ES, Garrett MR, Hopkins CR, Greka A. A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models. Science. 2017 Dec 8;358(6368):1332-1336. doi: 10.1126/science.aal4178. PMID: 29217578; PMCID: PMC6014699.

2: Chen L, Zhang Z, Tian H, Jiang S, Ji Y, Liu M, Shen J, Cao Z, Wang K. Synthesis of AC1903 analogs as potent transient receptor potential canonical channel 4/5 inhibitors and biological evaluation. Bioorg Med Chem. 2022 Aug 15;68:116853. doi: 10.1016/j.bmc.2022.116853. Epub 2022 May 27. PMID: 35653869.

3: Baradaran-Heravi A, Bauer CC, Pickles IB, Hosseini-Farahabadi S, Balgi AD, Choi K, Linley DM, Beech DJ, Roberge M, Bon RS. Nonselective TRPC channel inhibition and suppression of aminoglycoside-induced premature termination codon readthrough by the small molecule AC1903. J Biol Chem. 2022 Feb;298(2):101546. doi: 10.1016/j.jbc.2021.101546. Epub 2022 Jan 6. PMID: 34999117; PMCID: PMC8808171.

4: Sharma SH, Pablo JL, Montesinos MS, Greka A, Hopkins CR. Design, synthesis and characterization of novel N-heterocyclic-1-benzyl-1H-benzo[d]imidazole-2-amines as selective TRPC5 inhibitors leading to the identification of the selective compound, AC1903. Bioorg Med Chem Lett. 2019 Jan 15;29(2):155-159. doi: 10.1016/j.bmcl.2018.12.007. Epub 2018 Dec 4. PMID: 30538066; PMCID: PMC6349029.

5: Zhou Y, Kim C, Pablo JLB, Zhang F, Jung JY, Xiao L, Bazua-Valenti S, Emani M, Hopkins CR, Weins A, Greka A. TRPC5 Channel Inhibition Protects Podocytes in Puromycin-Aminonucleoside Induced Nephrosis Models. Front Med (Lausanne). 2021 Sep 21;8:721865. doi: 10.3389/fmed.2021.721865. PMID: 34621762; PMCID: PMC8490698.

6: Rubaiy HN. Treasure troves of pharmacological tools to study transient receptor potential canonical 1/4/5 channels. Br J Pharmacol. 2019 Apr;176(7):832-846. doi: 10.1111/bph.14578. Epub 2019 Mar 6. PMID: 30656647; PMCID: PMC6433652.

7: Pablo JL, Greka A. Charting a TRP to Novel Therapeutic Destinations for Kidney Diseases. Trends Pharmacol Sci. 2019 Dec;40(12):911-918. doi: 10.1016/j.tips.2019.10.001. Epub 2019 Nov 5. PMID: 31704171; PMCID: PMC6884692.

8: Zhang W, Wang M, Lv W, White FA, Chen X, Obukhov AG. Long-Term Treatment with Gadopentetic Acid or Gadodiamide Increases TRPC5 Expression and Decreases Adriamycin Nuclear Accumulation in Breast Cancer Cells. Cells. 2023 May 3;12(9):1304. doi: 10.3390/cells12091304. PMID: 37174704; PMCID: PMC10177392.

9: van der Wijst J, Bindels RJM. Renal physiology: TRPC5 inhibition to treat progressive kidney disease. Nat Rev Nephrol. 2018 Mar;14(3):145-146. doi: 10.1038/nrneph.2018.4. Epub 2018 Jan 22. PMID: 29355170.

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