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Fig. 1 · Structure
Cat. No.
A11143
CAS No.
501951-42-4
Formula
C17H16BrF3N4O
Mol. Weight
428

Documents & Downloads

SB-705498

Cat. No. A11143 CAS 501951-42-4

TRPV1 antagonist

SB-705498 is a potent, selective and orally bioavailable TRPV1 antagonist.

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Biological Activity

Target & Activity

Target Activity Value
hTRPV1 pKi 7.6
hTRPV1 pIC50 7.1

In Vitro Studies

SB-705498 was evaluated in IEC-6/TRPV1 + cells at 0.1 μM for 24 h. LDH release showed no significant difference compared with the control. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

SB-705498 and LDH release

Cell-based study · IEC-6/TRPV1 + [1]

IEC-6/TRPV1 + cells were treated with SB-705498 at 0.1 μM for 24 h. LDH release showed no significant difference compared with the control.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
LDH releaseReported result SB-705498 (0.1 μM), 24 h: 0.423 ± 0.149 gprot⋅mL -1; there was not any significant difference in LDH release compared with the control.[1]

Literature-Reported Treatment Conditions

Treatment concentration
0.1 μM
Exposure duration
24 h
Reported limits
Not stated in the sentences used: route, vehicle. Removed after verification: value.
Methods and source locations

Compound reported in the paper: SB-705498

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Characterization of TRPV1-Overexpressing (IEC-6/TRPV1+) and TRPV1-Knockdown (IEC-6/TRPV1-) Intestinal Epithelium Cell Lines 6 (S109); Table 3 legend (S184); Table 3 (T3.h1, T3.h2, T3.h3, T3.r3)

LDH release: LDH release; comparator: Cells treated with 1% ethyl alcohol in 10% culture medium — Results > Characterization of TRPV1-Overexpressing (IEC-6/TRPV1+) and TRPV1-Knockdown (IEC-6/TRPV1-) Intestinal Epithelium Cell Lines 6 (S109); Table 3 (T3.h1, T3.h2, T3.h3, T3.r3)

In Vivo Studies

In P19–21 F1.Scn1a +/− mice, subchronic SB-705498 treatment delivered orally at 500 mg SB-705498/kg chow did not affect spontaneous seizure frequency compared with control chow. Treatment with 500 mg/kg SB-705498 supplemented chow also did not affect seizure severity, assessed by the proportion of GTCS with full hindlimb extension. [2]

Spontaneous seizure frequency in mice

Animal study · P19–21 F1.Scn1a +/− mice [2]

In P19–21 F1.Scn1a +/− mice, subchronic SB-705498 treatment delivered orally through chow at 500 mg SB-705498/kg chow did not affect spontaneous seizure frequency compared with control chow.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
spontaneous seizure frequencyspontaneous seizure frequency 0.11 ± 0.03/h[2]

Conditions shared by the study groups

Route
orally through supplementation in chow
Treatment course
initiated following the induction of a single hyperthermia-induced GTCS on P18
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
SB-705498 500 mg SB-705498/kg chowcontrol chowSB-705498 subchronic treatment did not affect spontaneous seizure frequency, with n = 16–18 per treatment (control chow = 0.06 ± 0.03/h, 500 mg SB-705498/kg chow = 0.11 ± 0.03/h; p = 0.2, unpaired t-test).[2]
SB-705498 500 mg SB-705498/kg chow
Model: P19–21 F1.Scn1a +/− mice
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: SB-705498

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Spontaneous Seizures (S30, S31); Results > Trpv1 Receptor Inhibition does not Protect Against Hyperthermia-Induced and Spontaneous Seizures in F1.Scn1a +/− Mice (S71); FIGURE 2 legend (S101, S103, S105)

spontaneous seizure frequency: spontaneous seizure frequency; comparator: control chow — FIGURE 2 legend (S105)

SB-705498 500 mg SB-705498/kg chow · Results > Trpv1 Receptor Inhibition does not Protect Against Hyperthermia-Induced and Spontaneous Seizures in F1.Scn1a +/− Mice (S71); FIGURE 2 legend (S103, S105)

Seizure severity assessed by full hindlimb extension

Animal study · P19–21 F1.Scn1a +/− mice [2]

In P19–21 F1.Scn1a +/− mice, subchronic oral treatment with 500 mg/kg SB-705498 supplemented chow did not affect seizure severity compared with control chow, assessed by the proportion of GTCS with full hindlimb extension.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
proportion of GTCS with full hindlimb extensionseizure severity 23 hindlimb seizures of 88 seizures, 26%[2]

Conditions shared by the study groups

Route
orally through supplementation in chow
Treatment course
initiated following the induction of a single hyperthermia-induced GTCS on P18
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
SB-705498 500 mg/kg SB-705498 supplemented chowcontrol chowSeizure severity was not affected by subchronic SB-705498 treatment, with n = 16–18 per group (control chow = 9 hindlimb seizures of 45 seizures, 20%; 500 mg/kg SB-705498 supplemented chow = 23 hindlimb seizures of 88 seizures, 26%; p = 0.7, Chi-square test).[2]
SB-705498 500 mg/kg SB-705498 supplemented chow
Model: P19–21 F1.Scn1a +/− mice
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: SB-705498

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and Methods > Spontaneous Seizures (S30, S31); Results > Trpv1 Receptor Inhibition does not Protect Against Hyperthermia-Induced and Spontaneous Seizures in F1.Scn1a +/− Mice (S71, S74); FIGURE 2 legend (S101, S103, S107)

proportion of GTCS with full hindlimb extension: proportion of GTCS with full hindlimb extension; comparator: control chow — Results > Trpv1 Receptor Inhibition does not Protect Against Hyperthermia-Induced and Spontaneous Seizures in F1.Scn1a +/− Mice (S74); FIGURE 2 legend (S107)

SB-705498 500 mg/kg SB-705498 supplemented chow · FIGURE 2 legend (S103, S107)

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 501951-42-4
Applications TRPV1 antagonist
Formula C17H16BrF3N4O
Molecular Weight 428
SMILES
C1CN(C[C@@H]1NC(=O)NC2=CC=CC=C2Br)C3=NC=C(C=C3)C(F)(F)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 78 mg/mL (181.71 mM)
Water Insoluble
Ethanol 18 mg/mL (41.93 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Liang Q, Lv X, Cai Q, et al. Novobiocin, a Newly Found TRPV1 Inhibitor, Attenuates the Expression of TRPV1 in Rat Intestine and Intestinal Epithelial Cell Line IEC-6. Front Pharmacol (2018). PMID: 30374305 DOI: 10.3389/fphar.2018.01171 Source material
  2. [2] Satpute Janve V, Anderson LL, Bahceci D, et al. The Heat Sensing Trpv1 Receptor Is Not a Viable Anticonvulsant Drug Target in the Scn1a +/- Mouse Model of Dravet Syndrome. Front Pharmacol (2021). PMID: 34079465 DOI: 10.3389/fphar.2021.675128 Source material

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