2. Immunology/Inflammation
  3. Toll-like Receptor (TLR) IFNAR
  4. SM-276001

SM-276001 is a potent selective TLR7 agonist that can induce antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer.

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SM-276001 Chemical Structure

SM-276001 Chemical Structure

CAS No. : 473930-22-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

SM-276001 Related Antibodies

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Description

SM-276001 is a potent selective TLR7 agonist that can induce antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer[1][2].

IC50 & Target

TLR7; IFN[1][2]
Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
32 nM
Compound: 2
Agonist activity at human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay
Agonist activity at human TLR7 expressed in HEK293 cells by NFkappaB SEAP reporter gene assay
[PMID: 23265901]
In Vitro

SM-276001 (1 nM-10 μM) dose-dependently activates NF-κB through human TLR7[2].

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

SM-276001 Related Antibodies
In Vivo

SM-276001 demonstrates potent IFN-inducing activity at a dose of 0.1 mg/kg by oral administration in mice[1].
Oral administration of SM-276001, leads to the induction of an inflammatory cytokine and chemokine milieu and to the activation of a diverse population of immune effector cells including T and B lymphocytes, NK and NKT cells[2].
SM-276001 (3 mg/kg PO biweekly) significantly inhibits tumor growth in the Renca renal cell cancer and CT26 colorectal models[2].
SM-276001 (orally; 0.1, 1 or 10 mg/kg) leads to the activation of a diverse population of spleen-resident immune effector cells in Balb/c and C57BL/6J mice. When administered at 1 mg/kg or greater, the plasma concentration of SM-276001 exceeds the MEC of 30 nM[2].

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

Animal Model: C57BL/6 and B6C3F1 mice bearing Renca or CT26 tumors[2]
Dosage: 3 mg/kg
Administration: Oral administration twice weekly for 25 days
Result: Significantly reduced disease burden in mice bearing either Renca or CT26 tumors.
Molecular Weight

327.38

Formula

C16H21N7O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

NC1=C2C(N(C(N2)=O)CC3=CN=C(C=C3)C)=NC(NCCCC)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (381.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0546 mL 15.2728 mL 30.5455 mL
5 mM 0.6109 mL 3.0546 mL 6.1091 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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (6.35 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.35 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.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0546 mL 15.2728 mL 30.5455 mL 76.3639 mL
5 mM 0.6109 mL 3.0546 mL 6.1091 mL 15.2728 mL
10 mM 0.3055 mL 1.5273 mL 3.0546 mL 7.6364 mL
15 mM 0.2036 mL 1.0182 mL 2.0364 mL 5.0909 mL
20 mM 0.1527 mL 0.7636 mL 1.5273 mL 3.8182 mL
25 mM 0.1222 mL 0.6109 mL 1.2218 mL 3.0546 mL
30 mM 0.1018 mL 0.5091 mL 1.0182 mL 2.5455 mL
40 mM 0.0764 mL 0.3818 mL 0.7636 mL 1.9091 mL
50 mM 0.0611 mL 0.3055 mL 0.6109 mL 1.5273 mL
60 mM 0.0509 mL 0.2545 mL 0.5091 mL 1.2727 mL
80 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9545 mL
100 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7636 mL
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SM-276001 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SM-276001473930-22-2SM276001SM 276001Toll-like Receptor (TLR)IFNARInterferon-α/β receptorInterferon-alpha/beta receptorTLR7antitumorimmuneinterferonIFNInhibitorinhibitorinhibit

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