diABZI STING agonist-1 trihydrochloride

Name: diABZI STING agonist-1 trihydrochloride
Brand: MedChemExpress
SKU: HY-112921B
Rating: 5.0 (20 reviews)

Cat. No.: HY-112921B Purity: 98.54%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

For research use only. We do not sell to patients.

diABZI STING agonist-1 trihydrochloride Chemical Structure

CAS No. : 2138299-34-8

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 791	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 791	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 214	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3840	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of diABZI STING agonist-1 trihydrochloride:

diABZI STING agonist-1 In-stock
diABZI STING agonist-1 (Tautomerism) Get quote

20 Publications Citing Use of MCE diABZI STING agonist-1 trihydrochloride

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Biological Activity
Purity & Documentation
References
Customer Review

Description

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

IC₅₀ & Target

STING^[1].

In Vitro

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively. At a concentration of 1 μM, diABZI STING agonist-1 (compound 3) demonstrates high selectivity against more than 350 kinases tested^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

diABZI STING agonist-1 trihydrochloride (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo^[1].
diABZI STING agonist-1 trihydrochloride (intravenous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC₅₀) for mouse STING (200 ng/ml)^[1].
diABZI STING agonist-1 trihydrochloride (intravenous injection; 1.5 mg/kg; days 1, 4 and 8; 43 days) results in significant tumour growth inhibition and significantly improves survival (P < 0.001) with 8 out of 10 mice remaining tumor free at the end of the study on day 43^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Wild and Sting^−/− C57Blk6 mice^[1]
Dosage:	2.5 mg/kg
Administration:	Subcutaneous injection; 2.5 mg/kg
Result:	Activated secretion of IFNβ, IL-6, TNF, and CXCL1 in wild-type but not Sting^−/− mice.

Animal Model:	Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice^[1]
Dosage:	3 mg/kg
Administration:	Intravenous injection; 3 mg/kg
Result:	Exhibited a half-life of 1.4 hours and achieved systemic concentrations greater than EC₅₀ for mouse STING (200 ng/ml).

Animal Model:	Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice^[1]
Dosage:	1.5 mg/kg
Administration:	Intravenous injection; 1.5 mg/kg; 43 days
Result:	Resulted in significant tumour growth inhibition and improved survival.

Molecular Weight

959.32

Formula

C₄₂H₅₄Cl₃N₁₃O₇

CAS No.

2138299-34-8

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CC(C)=NN1CC)NC2=NC3=CC(C(N)=O)=CC(OC)=C3N2C/C=C/CN4C5=C(OCCCN6CCOCC6)C=C(C(N)=O)C=C5N=C4NC(C7=CC(C)=NN7CC)=O.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 90 mg/mL (93.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (26.06 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.0424 mL	5.2120 mL	10.4241 mL
5 mM	0.2085 mL	1.0424 mL	2.0848 mL
10 mM	0.1042 mL	0.5212 mL	1.0424 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (2.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 33.33 mg/mL (34.74 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (287 KB) SDS (0 KB)

COA (265 KB) HNMR (474 KB) RP-HPLC (242 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Ramanjulu JM, et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Nov 7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.0424 mL	5.2120 mL	10.4241 mL	26.0601 mL
	5 mM	0.2085 mL	1.0424 mL	2.0848 mL	5.2120 mL
	10 mM	0.1042 mL	0.5212 mL	1.0424 mL	2.6060 mL
	15 mM	0.0695 mL	0.3475 mL	0.6949 mL	1.7373 mL
	20 mM	0.0521 mL	0.2606 mL	0.5212 mL	1.3030 mL
	25 mM	0.0417 mL	0.2085 mL	0.4170 mL	1.0424 mL
DMSO	30 mM	0.0347 mL	0.1737 mL	0.3475 mL	0.8687 mL
	40 mM	0.0261 mL	0.1303 mL	0.2606 mL	0.6515 mL
	50 mM	0.0208 mL	0.1042 mL	0.2085 mL	0.5212 mL
	60 mM	0.0174 mL	0.0869 mL	0.1737 mL	0.4343 mL
	80 mM	0.0130 mL	0.0652 mL	0.1303 mL	0.3258 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.