IOWH032
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510267

CAS#: 1191252-49-9

Description: IOWH032 is a CFTR inhibitor. Diarrhea, a disease of poverty and poor sanitation, kills an estimated two million children each year. Oral rehydration therapy is a very simple and inexpensive treatment that has significantly reduced mortality from secretory diarrhea caused by rotavirus, cholera and enterotoxigenic Escherichia coli. The efficacy and adoption of oral rehydration therapy would be enhanced by a drug that reduces fluid loss associated with these diseases and alleviates disease symptoms. Secretion and absorption by the intestine offer a number of potential drug targets to reduce fluid loss.


Chemical Structure

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IOWH032
CAS# 1191252-49-9

Theoretical Analysis

MedKoo Cat#: 510267
Name: IOWH032
CAS#: 1191252-49-9
Chemical Formula: C22H15Br2N3O4
Exact Mass: 542.94
Molecular Weight: 545.187
Elemental Analysis: C, 48.47; H, 2.77; Br, 29.31; N, 7.71; O, 11.74

Price and Availability

Size Price Availability Quantity
50mg USD 150
100mg USD 250
200mg USD 450
500mg USD 950 2 Weeks
1g USD 1650 2 Weeks
2g USD 2650 2 Weeks
5g USD 3850 2 Weeks
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Synonym: IOWH032; IOWH-032; IOWH 032.

IUPAC/Chemical Name: 3-(3,5-dibromo-4-hydroxyphenyl)-N-(4-phenoxybenzyl)-1,2,4-oxadiazole-5-carboxamide .

InChi Key: DSFNLJXHXBIKDS-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H15Br2N3O4/c23-17-10-14(11-18(24)19(17)28)20-26-22(31-27-20)21(29)25-12-13-6-8-16(9-7-13)30-15-4-2-1-3-5-15/h1-11,28H,12H2,(H,25,29)

SMILES Code: O=C(C1=NC(C2=CC(Br)=C(O)C(Br)=C2)=NO1)NCC3=CC=C(OC4=CC=CC=C4)C=C3

Appearance: white to 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

More Info:          

Product Data:
Biological target: IOWH-032 is a a synthetic anti-secretory molecule, is a potent CFTR inhibitor with an IC50 value of 8 µM. IOWH-032 also is a anti-diarrheal agent.
In vitro activity: This study compared the supernatant viral loads of WT and ΔF CFBE41o- cells with that of IOWH-032-treated CFBE41o- WT cells at 24, 48 and 72 hpi by multiplex real-time RT-PCR. Remarkably, at 24 hpi, IOWH-032-treated CFBE41o- WT cells showed significantly lower viral loads than untreated WT and ΔF CFBE41o- cells. Moreover, at 72 hpi, the decrease in SARS-CoV-2 viral load in IOWH-032-treated CFBE41o- cells was significant (p < 0.0001) even when compared to the load in CFBE41o- ΔF cells (Figure 6a). Reference: Cells. 2022 Apr 15;11(8):1347. https://pubmed.ncbi.nlm.nih.gov/35456026/
In vivo activity: This study hypothesizes that insight into this question could be gained by comparing the effect of potentiators on CFTR channels from different origins, e.g., human, mouse, and Xenopus (frog). The present study combined this comparative molecular pharmacology approach with that of computer-aided drug discovery to identify and characterize new potentiators of CFTR and to explore possible mechanism of action. These results demonstrate that 1) VX-770, NPPB, GlyH-101, P1, P2, and P3 all exhibited ortholog-specific behavior in that they potentiated hCFTR, mCFTR, and xCFTR with different efficacies; 2) P1, P2, and P3 potentiated hCFTR in excised macropatches in a manner dependent on the degree of PKA-mediated stimulation; 3) P1 and P2 did not have additive effects, suggesting that these compounds might share binding sites. Also 4) using a pharmacophore modeling approach, this study identified three new potentiators (IOWH-032, OSSK-2, and OSSK-3) that have structures similar to GlyH-101 and that also exhibit ortholog-specific potentiation of CFTR. Reference: Am J Physiol Lung Cell Mol Physiol. 2016 Aug 1;311(2):L192-207. https://pubmed.ncbi.nlm.nih.gov/27288484/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 30.0 55.03
DMSO 76.7 140.62
DMSO:PBS (pH 7.2) (1:4) 0.2 0.37

Preparing Stock Solutions

The following data is based on the product molecular weight 545.19 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: 1. Lotti V, Merigo F, Lagni A, Di Clemente A, Ligozzi M, Bernardi P, Rossini G, Concia E, Plebani R, Romano M, Sbarbati A, Sorio C, Gibellini D. CFTR Modulation Reduces SARS-CoV-2 Infection in Human Bronchial Epithelial Cells. Cells. 2022 Apr 15;11(8):1347. doi: 10.3390/cells11081347. PMID: 35456026; PMCID: PMC9028056. 2. Cui G, Khazanov N, Stauffer BB, Infield DT, Imhoff BR, Senderowitz H, McCarty NA. Potentiators exert distinct effects on human, murine, and Xenopus CFTR. Am J Physiol Lung Cell Mol Physiol. 2016 Aug 1;311(2):L192-207. doi: 10.1152/ajplung.00056.2016. Epub 2016 Jun 10. PMID: 27288484; PMCID: PMC5142458.
In vitro protocol: 1. Lotti V, Merigo F, Lagni A, Di Clemente A, Ligozzi M, Bernardi P, Rossini G, Concia E, Plebani R, Romano M, Sbarbati A, Sorio C, Gibellini D. CFTR Modulation Reduces SARS-CoV-2 Infection in Human Bronchial Epithelial Cells. Cells. 2022 Apr 15;11(8):1347. doi: 10.3390/cells11081347. PMID: 35456026; PMCID: PMC9028056.
In vivo protocol: 1. Cui G, Khazanov N, Stauffer BB, Infield DT, Imhoff BR, Senderowitz H, McCarty NA. Potentiators exert distinct effects on human, murine, and Xenopus CFTR. Am J Physiol Lung Cell Mol Physiol. 2016 Aug 1;311(2):L192-207. doi: 10.1152/ajplung.00056.2016. Epub 2016 Jun 10. PMID: 27288484; PMCID: PMC5142458.

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1: de Hostos EL, Choy RK, Nguyen T. Developing novel antisecretory drugs to treat infectious diarrhea. Future Med Chem. 2011 Aug;3(10):1317-25. doi: 10.4155/fmc.11.87. Review. PubMed PMID: 21859305