DC Chemicals Limited
China
Product Name: Ethoxzolamide
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Purity: 98.0%
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 6-ETHOXY-2-BENZOTHIAZOLESULFONAMIDE
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Purity: 98.0%
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Contact: Ms Wang

452-35-7

452-35-7 structure

452-35-7 structure

Name: Ethoxzolamide
Chemical Name: ethoxzolamide
CAS Number: 452-35-7
Molecular Formula: C₉H₁₀N₂O₃S₂
Molecular Weight: 258.31700
Catalog: API Urinary system medication Diuretic
Create Date: 2018-09-27 02:37:44
Modify Date: 2024-01-08 12:04:54
Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.

Name	ethoxzolamide
Synonyms	Ethamide 6-ethoxy-1,3-benzothiazole-2-sulfonamide Glaucotensil Ethoxyzolamide Ethoxazolamide 2-Benzothiazolesulfonamide,6-ethoxy EINECS 207-199-5 MFCD00057089 Etoxzolamide 6-Ethoxy-2-benzothiazolesulfonamide Cardrase Diuretic C 6-ethoxybenzothiazole-2-sulphonamide

Description	Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Carbonic Anhydrase Research Areas >> Inflammation/Immunology Research Areas >> Infection
Target	Ki: 1 nM (carbonic anhydrase)[1]
In Vitro	Ethoxzolamide (ETZ) treatment causes >90% inhibition of reporter GFP fluorescence in infected macrophages. Moreover, in a 9-day macrophage survival assay, Ethoxzolamide (ETZ) treatment significantly inhibits the ability of M. tuberculosis to grow intracellularly[2].
In Vivo	It is discovered that the lipid-soluble ethoxzolamide is converted in vivo to a water-soluble metabolite, while retaining high activity againstt the enzyme. At the minimal dose for maximal effect (4 mg/kg i.v. at 45 min) the IOP lowering is 4.2 mmHg, the concentration in anterior uvea is 2.5 pmol/kg, and the fractional inhibition of the enzyme (i) is 0.9995. The effect declines rapidly, attributable to the very short half-life of drug in plasma, leading to depletion of free drug in the anterior uvea and other tissues[1]. Ethoxzolamide (ETZ) strongly downregulates GFP reporter fluorescence in mouse lungs, with 3-fold inhibition of GFP signal compare to that in the mock-treating control. There is a significant reduction of bacterial survival in the lungs of ETZ-treating mice compare to the mock-treating control[2].
Cell Assay	BMDMs are treated with 80 μM Ethoxzolamide (ETZ) or an equivalent volume of DMSO every 2 days for 9 days total. At days 3, 6, and 9, intracellular bacteria are quantified by lysing macrophage monolayers and performing serial dilution plating of lysates on 7H10 agar. For fluorescence microscopy experiments, macrophages are seeded on glass coverslips before infection with M. tuberculosis CDC1551. Samples are treated every 2 days with 100 μM Ethoxzolamide (ETZ) or an equal volume of DMSO for 9 days[2].
Animal Admin	Rats (male, 300–325 g) are randomly selected into 2 groups (n=6 each group) and Ethoxzolamide (EZ) is administered at a dose of 0.18 mg/kg (in PEG 300: ethanol, 1:1) via i.v. injection through the tail vein. Blood samples (about 50-100 µL) are collected in heparinizing tubes at 0, 15, 30, 60, 120, 180, 240, 360, 540, and 1440 min post-injection, via tail snip with isoflurane as anesthetic. Plasma samples are prepared and stored at -80 °C until analysis. To study the distribution in brain, rats in group 1 are scarified at 6 hours and rats in group 2 are scarified at 24 hours to collect the brain tissues. Those blood samples from group 2 are analyzed to generated PK profile[3].
References	[1]. Maren TH, et al. Relations among IOP reduction, ocular disposition and pharmacology of the carbonic anhydrase inhibitor ethoxzolamide. Exp Eye Res. 1992 Jul;55(1):73-9. [2]. Benjamin K. Johnson, et al. The Carbonic Anhydrase Inhibitor Ethoxzolamide Inhibits theMycobacterium tuberculosis PhoPR Regulon and Esx-1 Secretion and Attenuates Virulence. Antimicrob Agents Chemother. 2015 Aug; 59(8): 4436–4445. [3]. Song Gao, et al. Development and validation of an UPLC-MS/MS method for the quantification of ethoxzolamide in plasma and bioequivalent buffers: Applications to absorption, brain distribution, and pharmacokinetic studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Apr 1; 0: 54–59.

Density	1.47g/cm3
Boiling Point	464.9ºC at 760mmHg
Melting Point	190-193ºC(lit.)
Molecular Formula	C₉H₁₀N₂O₃S₂
Molecular Weight	258.31700
Flash Point	235ºC
Exact Mass	258.01300
PSA	118.90000
LogP	3.12350
Vapour Pressure	8.05E-09mmHg at 25°C
Index of Refraction	1.644
Storage condition	2-8℃

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DL6390000

CHEMICAL NAME :: 2-Benzothiazolesulfonamide, 6-ethoxy-

CAS REGISTRY NUMBER :: 452-35-7

BEILSTEIN REFERENCE NO. :: 0212240

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C9-H10-N2-O3-S2

MOLECULAR WEIGHT :: 258.33

WISWESSER LINE NOTATION :: T56 BN DSJ CSZW GO2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3300 mg/kg

SEX/DURATION :: female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 1,51,1968

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319-H335
Precautionary Statements	P261-P305 + P351 + P338
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xi: Irritant;
Risk Phrases	R36/37/38
Safety Phrases	26
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	DL6390000
HS Code	2935009090

5304-15-4 structure

5304-15-4

~87%

452-35-7 structure

452-35-7

Literature: Larsen, R.D.; Roberts, F.E. Synthetic Communications, 1986 , vol. 16, # 8 p. 899 - 904

Precursor 1
5304-15-4
DownStream 10
939-69-5 20240-21-5 34500-31-7 2591-17-5
20115-09-7 86394-92-5 86394-93-6 86394-98-1
88946-18-3 91634-13-8

HS Code	2935009090
Summary	2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%