2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. RN-1747

RN-1747 is a selective TRPV4 channel agonist, with EC50 values of 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1747 acts as an antagonist of TRPM8, with an IC50 of 4 μM. Topical cutaneous administration of RN-1747 induces hypothermia, increases tail heat loss via cutaneous vasodilation, and promotes cold-seeking behavior in rats. Intracerebroventricular administration of RN-1747 does not induce hypothermia in rats.

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RN-1747

RN-1747 Chemical Structure

CAS No. : 1024448-59-6

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Based on 5 publication(s) in Google Scholar

RN-1747 Related Antibodies

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

View All Isoforms
TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

RN-1747 is a selective TRPV4 channel agonist, with EC50 values of 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. RN-1747 acts as an antagonist of TRPM8, with an IC50 of 4 μM. Topical cutaneous administration of RN-1747 induces hypothermia, increases tail heat loss via cutaneous vasodilation, and promotes cold-seeking behavior in rats. Intracerebroventricular administration of RN-1747 does not induce hypothermia in rats[1][2].

IC50 & Target[1]

hTRPV4

0.77 μM (EC50)

rTRPV4

4.1 μM (EC50)

mTRPV4

4.0 μM (EC50)

TRPM8

4.0 μM (IC50)

In Vitro

RN-1747 (13 nM-30 μM; 10 min) activates T-REx HEK 293 cells expressing hTRPV4, with an EC50 of 0.77 μM[1].
RN-1747 (13 nM-30 μM; 10 min) activates T-REx HEK 293 cells expressing mouse TRPV4, with an EC50 of 4.0 μM[1].
RN-1747 (13 nM-30 μM; 10 min) activates T-REx HEK 293 cells expressing rat TRPV4, with an EC50 of 4.1 μM[1].
RN-1747 (10 μM) induces robust inward currents in Xenopus oocytes expressing hTRPV4, confirming its rapid-acting agonist activity[1].
RN-1747 acts as an antagonist of TRPM8 with an IC50 of 4 μM, and exhibits weak agonist activity against TRPV1 at an extremely high concentration of 100 μM[1].

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

RN-1747 Related Antibodies
In Vivo

RN-1747 (10-100 μg/kg, 500 μg/mL; intravenous, topical, intracerebroventricular administration) induces hypothermia via activation of peripheral TRPV4 when administered topically, induces hyperthermia when administered intracerebroventricularly, but exerts no significant effect on core body temperature when administered intravenously in male Wistar rats maintained at 26 °C[2].
Topical administration of RN-1747 (500 μg/mL) enhances the vasodilatory function of tail skin, which is manifested by a significant negative correlation between heat dissipation index and core body temperature, thereby inducing hypothermia in male Wistar rats at 26 °C[2].
RN-1747 (500 μg/mL; administered locally) abolishes the preference of male Wistar rats for a warm environment (32 °C) but not a thermoneutral environment (26 °C), indicating impairment of their heat-seeking behavior[2].
Topical administration of RN-1747 (1000 μg/mL) induces cold-seeking behavior in male Wistar rats, characterized by a significant reduction in preferred ambient temperature and a decrease in core body temperature in temperature gradient tests[2].
Topical administration of RN-1747 (1000 μg/mL) induces cold-seeking behavior in male Wistar rats, which is characterized by a significant reduction in preferred ambient temperature and a decrease in core body temperature in temperature gradient tests[2].

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

Animal Model: Wistar rats (male, 8-10 weeks old, 290-320 g)[2]
Dosage: 10 μg/kg (i.c.v.); 100 μg/kg (i.v.); 500 μg/mL (topical)
Administration: i.v.; infusion at 0.08 mL/min; 1 mL/kg volume; topical; 1 mL volume; i.c.v.; infusion at 0.8 μL/min; 4 μL/kg volume
Result: Did not produce a significant change in core body temperature compared to vehicle (F1,42=0.348; P=1.000).
Caused a significant decrease in core body temperature compared to vehicle (F1,42=1.786; P=0.002).
Had its hypothermic effect significantly inhibited by pre-treatment with RN-1734 (F1,42=1.482; P=0.028).
Caused a significant increase in core body temperature compared to vehicle (F1,42=2.351; P<0.001).
Animal Model: Wistar rats (male, 8-10 weeks old, 290-320 g)[2]
Dosage: 500 μg/mL
Administration: topical; 1 mL volume
Result: Showed a significant negative relationship between heat loss index and core body temperature (P=0.009, R2=0.221).
Had higher tail temperatures than untreated or vehicle-treated rats, indicating TRPV4 activation stimulated vasodilation.
Animal Model: Wistar rats (male, 8-10 weeks old, 290-320 g)[2]
Dosage: 500 μg/mL
Administration: topical; 2 mL volume
Result: Did not affect exploratory behaviour (crossings between plates: 26 vs 18 °C: P=0.738; 26 vs 32 °C: P=0.221).
Showed no significant preference between 26 °C and 32 °C (P=0.135), unlike vehicle-treated rats which preferred 32 °C over 26 °C (P=0.020).
Preferred 26 °C over 18 °C (P<0.001), similar to vehicle-treated rats (P=0.002).
Animal Model: Wistar rats (male, 8-10 weeks old, 290-320 g)[2]
Dosage: 1000 μg/mL
Administration: topical; 1 mL volume
Result: Caused a significant reduction in preferred ambient temperature compared to vehicle (F1,9=4.18; P<0.001).
Caused a reduction in core body temperature of up to 0.7 °C over time, while vehicle-treated rats had only a slight core body temperature change of 0.1 °C (F=1.41; P=0.02).
Molecular Weight

395.86

Formula

C17H18ClN3O4S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=S(N1CCN(CC2=CC=CC=C2)CC1)(C3=CC=C(Cl)C=C3[N+]([O-])=O)=O
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 : 50 mg/mL (126.31 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 2.5261 mL 12.6307 mL 25.2615 mL
5 mM 0.5052 mL 2.5261 mL 5.0523 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.

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

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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 (5.25 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 (5.25 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 2.5261 mL 12.6307 mL 25.2615 mL 63.1536 mL
5 mM 0.5052 mL 2.5261 mL 5.0523 mL 12.6307 mL
10 mM 0.2526 mL 1.2631 mL 2.5261 mL 6.3154 mL
15 mM 0.1684 mL 0.8420 mL 1.6841 mL 4.2102 mL
20 mM 0.1263 mL 0.6315 mL 1.2631 mL 3.1577 mL
25 mM 0.1010 mL 0.5052 mL 1.0105 mL 2.5261 mL
30 mM 0.0842 mL 0.4210 mL 0.8420 mL 2.1051 mL
40 mM 0.0632 mL 0.3158 mL 0.6315 mL 1.5788 mL
50 mM 0.0505 mL 0.2526 mL 0.5052 mL 1.2631 mL
60 mM 0.0421 mL 0.2105 mL 0.4210 mL 1.0526 mL
80 mM 0.0316 mL 0.1579 mL 0.3158 mL 0.7894 mL
100 mM 0.0253 mL 0.1263 mL 0.2526 mL 0.6315 mL
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RN-1747 Related Classifications

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  • 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:

RN-17471024448-59-6RN1747RN 1747TRP ChannelTransient receptor potential channelscentral TRPV4 channelsT-REx HEK 293 cellshuman TRPV4 channelsXenopus oocyteshuman TRPV1mouse TRPV4 channelshuman TRPM8rat TRPV4 channelsperipheral TRPV4 channelsTRPV4 channelInhibitorinhibitorinhibit

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