GlyH-101 | CAS#328541-79-3 | CFTR inhibitor

GlyH-101
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510335

CAS#: 328541-79-3

Description: GlyH-101 is a CFTR inhibitor (cystic fibrosis transmembrane conductance regulator). GlyH-101 is a glycine hydrazide that has been shown to block CFTR channels. GlyH-101 blocked I(Cl.PKA) in a concentration- and voltage-dependent fashion (IC(50) at +100 mV=0.3 Â± 1.5 μM and at -100 mV=5.1 Â± 1.3 μM). GlyH-101 blocks the open pore of cardiac CFTR channels at an electrical distance of 0.15 Â± 0.03 from the external membrane surface.

Chemical Structure

GlyH-101

CAS# 328541-79-3

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 510335
Name: GlyH-101
CAS#: 328541-79-3
Chemical Formula: C19H15Br2N3O3
Exact Mass: 490.95
Molecular Weight: 493.155
Elemental Analysis: C, 46.27; H, 3.07; Br, 32.41; N, 8.52; O, 9.73

Price and Availability

Size	Price	Availability
25mg	USD 150
50mg	USD 250
100mg	USD 450
200mg	USD 750
500mg	USD 1250
1g	USD 2050	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: GlyH101; GlyH 101; GlyH-101.

IUPAC/Chemical Name: (E)-N'-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(naphthalen-2-ylamino)acetohydrazide

InChi Key: RMBDLOATEPYBSI-NUGSKGIGSA-N

InChi Code: InChI=1S/C19H15Br2N3O3/c20-15-8-13(18(26)17(21)19(15)27)9-23-24-16(25)10-22-14-6-5-11-3-1-2-4-12(11)7-14/h1-9,22,26-27H,10H2,(H,24,25)/b23-9+

SMILES Code: O=C(N/N=C/C1=C(O)C(Br)=C(O)C(Br)=C1)CNC2=CC3=CC=CC=C3C=C2

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, 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:

Product Data

Instruction:

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Biological target:	GlyH-101 is a potent CFTR inhibitor.
In vitro activity:	On treatment with GlyH‐101, there appeared to be a redistribution of F‐actin from the periphery (Figure 4b,e). Profile analysis of the images using ImageJ confirmed a loss of cortical rim F‐actin to form cytosolic F‐actin polymers in cells treated with GlyH‐101 at 24 h under both static and shear conditions (Figure 4h). Furthermore, a significant (p < 0.05) increase in F‐actin (Figure 4g) and the occurrence of paracellular gaps (Figure 4e) after 24 h of shear stress was observed in cells treated with GlyH‐101, suggesting the formation of cytosolic stress fibers and cellular retraction, compared to cells treated with GlyH‐101 in static conditions. Reference: Physiol Rep. 2021 Dec;9(23):e15128. https://pubmed.ncbi.nlm.nih.gov/34851051/
In vivo activity:	GlyH-101 also decreased AHR in SPT-deficient mice in vivo. This study identifies the manipulation of sphingolipid synthesis as a novel metabolic therapeutic strategy to alleviate AHR. Reference: Am J Respir Cell Mol Biol. 2020 Nov;63(5):690-698. https://pubmed.ncbi.nlm.nih.gov/32706610/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	30.0	60.83
	DMF:PBS (pH 7.2) (1:1)	0.5	1.01
	DMSO	57.6	116.75

Preparing Stock Solutions

The following data is based on the product molecular weight 493.16 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. Causer AJ, Khalaf M, Klein Rot E, Brand K, Smith J, Bailey SJ, Cummings MH, Shepherd AI, Saynor ZL, Shute JK. CFTR limits F-actin formation and promotes morphological alignment with flow in human lung microvascular endothelial cells. Physiol Rep. 2021 Dec;9(23):e15128. doi: 10.14814/phy2.15128. PMID: 34851051; PMCID: PMC8634629. 2. Callaghan PJ, Ferrick B, Rybakovsky E, Thomas S, Mullin JM. Epithelial barrier function properties of the 16HBE14o- human bronchial epithelial cell culture model. Biosci Rep. 2020 Oct 30;40(10):BSR20201532. doi: 10.1042/BSR20201532. PMID: 32985670; PMCID: PMC7569203. 3. Heras AF, Veerappan A, Silver RB, Emala CW, Worgall TS, Perez-Zoghbi J, Worgall S. Increasing Sphingolipid Synthesis Alleviates Airway Hyperreactivity. Am J Respir Cell Mol Biol. 2020 Nov;63(5):690-698. doi: 10.1165/rcmb.2020-0194OC. PMID: 32706610; PMCID: PMC7605160.
In vitro protocol:	1. Causer AJ, Khalaf M, Klein Rot E, Brand K, Smith J, Bailey SJ, Cummings MH, Shepherd AI, Saynor ZL, Shute JK. CFTR limits F-actin formation and promotes morphological alignment with flow in human lung microvascular endothelial cells. Physiol Rep. 2021 Dec;9(23):e15128. doi: 10.14814/phy2.15128. PMID: 34851051; PMCID: PMC8634629. 2. Callaghan PJ, Ferrick B, Rybakovsky E, Thomas S, Mullin JM. Epithelial barrier function properties of the 16HBE14o- human bronchial epithelial cell culture model. Biosci Rep. 2020 Oct 30;40(10):BSR20201532. doi: 10.1042/BSR20201532. PMID: 32985670; PMCID: PMC7569203.
In vivo protocol:	1. Heras AF, Veerappan A, Silver RB, Emala CW, Worgall TS, Perez-Zoghbi J, Worgall S. Increasing Sphingolipid Synthesis Alleviates Airway Hyperreactivity. Am J Respir Cell Mol Biol. 2020 Nov;63(5):690-698. doi: 10.1165/rcmb.2020-0194OC. PMID: 32706610; PMCID: PMC7605160.

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1: Melis N, Tauc M, Cougnon M, Bendahhou S, Giuliano S, Rubera I, Duranton C. Revisiting CFTR inhibition: a comparative study of CFTRinh -172 and GlyH-101 inhibitors. Br J Pharmacol. 2014 Aug;171(15):3716-27. doi: 10.1111/bph.12726. PubMed PMID: 24758416; PubMed Central PMCID: PMC4128068.

2: Norimatsu Y, Ivetac A, Alexander C, O'Donnell N, Frye L, Sansom MS, Dawson DC. Locating a plausible binding site for an open-channel blocker, GlyH-101, in the pore of the cystic fibrosis transmembrane conductance regulator. Mol Pharmacol. 2012 Dec;82(6):1042-55. doi: 10.1124/mol.112.080267. Epub 2012 Aug 24. PubMed PMID: 22923500; PubMed Central PMCID: PMC3502623.

3: Sheppard DN. CFTR channel pharmacology: insight from a flock of clones. Focus on "Divergent CFTR orthologs respond differently to the channel inhibitors CFTRinh-172, glibenclamide, and GlyH-101". Am J Physiol Cell Physiol. 2012 Jan 1;302(1):C24-6. doi: 10.1152/ajpcell.00376.2011. Epub 2011 Oct 12. PubMed PMID: 21998142.

4: Stahl M, Stahl K, Brubacher MB, Forrest JN Jr. Divergent CFTR orthologs respond differently to the channel inhibitors CFTRinh-172, glibenclamide, and GlyH-101. Am J Physiol Cell Physiol. 2012 Jan 1;302(1):C67-76. doi: 10.1152/ajpcell.00225.2011. Epub 2011 Sep 21. PubMed PMID: 21940661; PubMed Central PMCID: PMC3328903.

5: Barman PP, Choisy SC, Gadeberg HC, Hancox JC, James AF. Cardiac ion channel current modulation by the CFTR inhibitor GlyH-101. Biochem Biophys Res Commun. 2011 Apr 29;408(1):12-7. doi: 10.1016/j.bbrc.2011.03.089. Epub 2011 Mar 31. PubMed PMID: 21439936.

6: Kelly M, Trudel S, Brouillard F, Bouillaud F, Colas J, Nguyen-Khoa T, Ollero M, Edelman A, Fritsch J. Cystic fibrosis transmembrane regulator inhibitors CFTR(inh)-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition. J Pharmacol Exp Ther. 2010 Apr;333(1):60-9. doi: 10.1124/jpet.109.162032. Epub 2010 Jan 5. PubMed PMID: 20051483.

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