| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
Purity: ≥98%
DHQZ-36 is a novel and potent small molecule retrograde trafficking inhibitor which is able to block infection by several human and monkey polyomaviruses. It acts by protecting cells from infections by human polyoma- and papillomaviruses. DHQZ-3 represents an advance in the development of drug candidates that can broadly protect humans from non-enveloped DNA viruses and toxins that exploit retrograde trafficking as a means for cell entry. Human polyoma- and papillomaviruses are non-enveloped DNA viruses that cause severe pathologies and mortalities. Under circumstances of immunosuppression, JC polyomavirus causes a fatal demyelinating disease called progressive multifocal leukoencephalopathy (PML) and the BK polyomavirus is the etiological agent of polyomavirus-induced nephropathy and hemorrhagic cystitis. Human papillomavirus type 16, another non-enveloped DNA virus, is associated with the development of cancers in tissues like the uterine cervix and oropharynx. Currently, there are no approved drugs or vaccines to treat or prevent polyomavirus infections.
| Targets |
Leishmania amazonensis(EC50=13.63 μM)
|
|---|---|
| ln Vitro |
The size of parasitophorous vacuoles (LPVs) decreases significantly with increasing concentrations of DHQZ 36; at 50 μM, vacuole sizes are reduced by 30%. There is a decrease in the quantity of parasites for every macrophage due to these parasites. After using DHQZ 36, significant parasite loss is seen at as low as 5 μM. When DHQZ 36 is applied at concentrations of 12.5 μM or higher, parasites cannot grow again.
Over 40% less parasite protein is secreted when DHQZ 36 is present. After LPS activation, DHQZ 36 reverses the suppression of IL-6 release by infected cells caused by Leishmania[1]. |
| References |
| Molecular Formula |
C21H18F2N2OS
|
|---|---|
| Molecular Weight |
384.442230701447
|
| Exact Mass |
384.11
|
| Elemental Analysis |
C, 65.61; H, 4.72; F, 9.88; N, 7.29; O, 4.16; S, 8.34
|
| CAS # |
1542098-94-1
|
| Related CAS # |
1542098-94-1;
|
| PubChem CID |
72720908
|
| Appearance |
Solid powder
|
| LogP |
5
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
27
|
| Complexity |
528
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SVXVTSKHYHQIPJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H18F2N2OS/c1-2-16-8-10-19(27-16)20-24-18-9-7-15(23)11-17(18)21(26)25(20)12-13-3-5-14(22)6-4-13/h3-11,20,24H,2,12H2,1H3
|
| Chemical Name |
2-(5-Ethyl-thiophen-2-yl)-6-fluoro-3-(4-fluoro-benzyl)-2,3-dihydro-1H-quinazolin-4-one
|
| Synonyms |
DHQZ-36; DHQZ 36; DHQZ36;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6012 mL | 13.0059 mL | 26.0119 mL | |
| 5 mM | 0.5202 mL | 2.6012 mL | 5.2024 mL | |
| 10 mM | 0.2601 mL | 1.3006 mL | 2.6012 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
