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Fig. 1 · Structure
Cat. No.
A10313
CAS No.
16208-51-8
Formula
C4H8Na2O6S4
Mol. Weight
326.3

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Dimesna (BNP7787)

Cat. No. A10313 CAS 16208-51-8

Protective agent

Dimesna is an uroprotective agent used to decrease urotoxicity.

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Biological Activity

Bioactivity / Mechanism

Dimesna (BNP7787) acts as an alternative substrate in purified thioredoxin- and glutaredoxin-coupled systems. Cofactor and enzyme omission controls distinguish this turnover from direct reductase activity. These experiments do not establish cellular inhibitory potency. [1,2]

After protein pretreatment and removal of free BNP7787, thioredoxin and peroxiredoxin 1 showed reduced coupled enzyme activity relative to processed buffer controls. Free BNP7787 itself drives NADPH turnover, making its removal essential for interpreting these assays. [1,2]

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

In Vitro Studies

BNP7787 turnover in the coupled thioredoxin system

Biochemical assay · Human Trx with TrxR/NADPH, with and without Trx [1]

BNP7787 supported substantially more NADPH oxidation with Trx present than with TrxR alone; the no-disulfide background was retained.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
NADPH oxidation with BNP7787; Reaction A (TrxR alone), Reaction B (+Trx), and no-disulfide controlsnmoles/min/mL BNP7787: A 0.3 ± 0.01; B 13.1 ± 0.2. No disulfide: A 0.14 ± 0.01; B 0.30 ± 0.04.[1]

Literature-Reported Treatment Conditions

Treatment concentration
0.5 mM BNP7787
Exposure duration
Initial 4-minute linear assay interval
Method
Coupled enzyme assay at 25 °C with 200 µM NADPH and 4.8 µM human Trx when included
Vehicle
Potassium phosphate assay buffer, pH 7.0
Co-treatment
TrxR and NADPH; no cytotoxic drug
Reported limits
Materials lists rat TrxR, while assay method specifies bovine TrxR; species discrepancy retained.
Methods and source locations

Compound reported in the paper: Dimesna; Compound label in the paper: BNP7787

Compound-level evidence only; no Adooq lot validation or interchangeability with mesna or free acid.

Table 1 (BNP7787 and no-disulfide rows, footnotes a–c); Methods: Evaluating the Effect of BNP7787 ... on Thioredoxin and Thioredoxin Reductase Activity Assays; Results: alternative substrates

NADPH oxidation with BNP7787; Reaction A (TrxR alone), Reaction B (+Trx), and no-disulfide controls: Table values; triplicate or more assays; first 4-minute absorbance change. Meaning of ± not defined in table footnote. — Table 1 (BNP7787 and no-disulfide rows, footnotes a–c); Methods: Evaluating the Effect of BNP7787 ... on Thioredoxin and Thioredoxin Reductase Activity Assays; Results: alternative substrates

Activity of BNP7787-treated thioredoxin after free compound removal

Biochemical assay · Wild-type human Trx, insulin-disulfide reduction assay [1]

BNP7787-treated Trx showed lower coupled insulin-reduction activity after removal of small molecules; buffer and glutathione-disulfide preparations underwent the same workup.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
NADPH oxidation relative to buffer-treated Trx% of Trx control rate At 1.75 µg Trx: BNP7787-treated 65.9%, GSH-adduct control 62.5%; at 3.5 µg Trx: 74.6% and 78.0%, respectively; buffer controls 100.0%.[1]

Literature-Reported Treatment Conditions

Treatment concentration
10 mM BNP7787 during protein modification
Exposure duration
4 h at 37 °C, followed by small-molecule removal before activity assay
Method
Reduced WT Trx treated with BNP7787, glutathione disulfide or buffer; all passed through PD Spin Traps
Vehicle
Tris buffer, pH 8.0
Co-treatment
Insulin as activity substrate; glutathione disulfide 10 mM as comparator
Reported limits
Figure does not define error bars; protein amounts are assay loads, not compound doses.
Methods and source locations

Compound reported in the paper: Dimesna; Compound label in the paper: BNP7787

Compound-level evidence only; no Adooq lot validation or interchangeability with mesna or free acid.

Figure 3A–D (PDF p8); Methods: Preparation of BNP7787-modified Trx for Evaluation in Thioredoxin Activity Assays and Native Gel Electrophoresis; Results: decreased rate

NADPH oxidation relative to buffer-treated Trx: Printed Figure 3A labels; triplicate reactions. Error-bar definition not specified in caption. — Figure 3A–D (PDF p8); Methods: Preparation of BNP7787-modified Trx for Evaluation in Thioredoxin Activity Assays and Native Gel Electrophoresis; Results: decreased rate

BNP7787 as a substrate in a glutaredoxin-coupled assay

Biochemical assay · Recombinant human Grx1 with glutathione reductase, NADPH and GSH omission controls [2]

The highest BNP7787-associated NADPH oxidation rate required Grx plus GSH; glutathione reductase alone showed negligible turnover.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
NADPH oxidation in three enzyme/cofactor conditionsnmoles/min/mL Grx + GSH: 15.3 ± 1.0; GSH without Grx: 2.9 ± 1.6; neither Grx nor GSH: 0.0 ± 0.01.[2]

Literature-Reported Treatment Conditions

Treatment concentration
0.5 mM BNP7787
Exposure duration
10 min at room temperature; rate from linear portion of first 4 min
Method
340 nm coupled assay; 50 nM glutathione reductase, 400 µM NADPH; Grx/GSH included or omitted
Vehicle
Tris-Cl, pH 8.0
Co-treatment
1 mM GSH where included; no cytotoxic drug
Reported limits
No cellular potency endpoint; ± statistic not defined in Table 1.
Methods and source locations

Compound reported in the paper: Dimesna; Compound label in the paper: BNP7787

Compound-level evidence only; no Adooq lot validation or interchangeability with mesna or free acid.

Section 2.1, Table 1 BNP7787 row and footnotes; Sections 3.1–3.2

NADPH oxidation in three enzyme/cofactor conditions: Table 1; average of at least two independent experiments performed in triplicate (reported n = 6). The table does not define the ± statistic. — Section 2.1, Table 1 BNP7787 row and footnotes; Sections 3.1–3.2

Peroxiredoxin activity after BNP7787 treatment

Biochemical assay · Human Prx1 in a Trx/TrxR-coupled peroxide assay [2]

BNP7787-treated Prx1 retained less activity than identically processed buffer-treated Prx1 after free BNP7787 was removed.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Peroxide-triggered NADPH oxidation relative to apo-Prx% of control At 4.8 µM Prx: 76.5% (p<.05); at 2.4 µM Prx: 57.2% (p<.001); respective apo-Prx controls 100.0%.[2]

Literature-Reported Treatment Conditions

Treatment concentration
20 mM BNP7787 during Prx1 pretreatment; 4.8 or 2.4 µM Prx1 in subsequent assay
Exposure duration
Pretreatment 16 h at 37 °C; assay monitored 30 min at 25 °C, rate from a 4-minute linear segment
Method
Reduced Prx1 incubated with BNP7787 or buffer; both processed by G25 chromatography before coupled assay
Vehicle
NH4HCO3 pretreatment buffer; HEPES assay buffer
Co-treatment
Human Trx1 and rat liver TrxR coupling enzymes; 100 µM H2O2 initiates assay
Reported limits
Figure caption does not define n or error bars. Pretreatment concentration is not an IC50.
Methods and source locations

Compound reported in the paper: Dimesna; Compound label in the paper: BNP7787

Compound-level evidence only; no Adooq lot validation or interchangeability with mesna or free acid.

Section 2.4, Figure 3A–C; Sections 3.1 and 3.3

Peroxide-triggered NADPH oxidation relative to apo-Prx: Printed Figure 3C values. Bars also show no-Prx/no-H2O2 and no-H2O2 protein backgrounds; error-bar definition and n not given in caption. — Section 2.4, Figure 3A–C; Sections 3.1 and 3.3

In Vivo Studies

In WARD tumour-bearing Fischer rats given a single intravenous BNP7787 dose, mesna exposure was higher in kidney than plasma. Compared with equal-mass mesna dosing, BNP7787 produced lower plasma mesna exposure, while the tumour exposure difference was not statistically significant. This distribution study did not directly test cisplatin nephroprotection. [3]

Comparative BNP7787 and mesna tissue pharmacokinetics

Animal study · Female Fischer rats bearing subcutaneous WARD colorectal tumours [3]

BNP7787 dosing produced higher mesna exposure in kidney than plasma; plasma mesna exposure was lower than after equal-mass mesna dosing. This experiment measured distribution, not protection against a concurrent cisplatin challenge.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Mesna exposure following BNP7787 versus mesna dosingAUC5–t comparison After BNP7787: kidney/plasma mesna AUC ratio 4.5. Plasma mesna AUC was five-fold lower than after mesna dosing (P<0.01). Tumour mesna AUC was 2.1-fold lower, not statistically significant.[3]

Conditions shared by the study groups

Route
Intravenous tail vein
Frequency
Single bolus
Treatment course
Sampling at 0, 5, 15, 30, 45, 60, 90 and 150 min
Vehicle
Water for injection; 200 mg/mL drug solution
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
BNP7787
1000 mg kg−1		Parallel group receiving the other compound at the same mass doseKidney/plasma mesna AUC ratio 4.5; lower plasma mesna AUC than after mesna.[3]
Mesna comparator
1000 mg kg−1		Parallel group receiving the other compound at the same mass dosePlasma mesna AUC five-fold higher than after BNP7787; tumour difference nonsignificant.[3]
BNP7787
Model: Female Fischer rats bearing subcutaneous WARD colorectal tumours
Reported limits: No concurrent chemotherapy challenge; n is per terminal sampling time, not repeated measurements in one rat.
Mesna comparator
Model: Female Fischer rats bearing subcutaneous WARD colorectal tumours
Reported limits: No concurrent chemotherapy challenge; n is per terminal sampling time, not repeated measurements in one rat.
Methods and source locations

Compound reported in the paper: Dimesna; Compound label in the paper: BNP7787

Compound-level evidence only; no Adooq lot validation or interchangeability with mesna or free acid.

Materials and Methods: Drug solutions, Animals, Sampling, Sample analysis, Pharmacokinetic and statistical analysis; Results: BNP7787 administration and BNP7787 vs mesna administration; Figures 3–4; Discussion (AUC limitations)

Mesna exposure following BNP7787 versus mesna dosing: Selective micro-HPLC/dual electrochemical detection; AUC from 5 min to last quantifiable sample or 150 min; no extrapolation to infinity. — Materials and Methods: Drug solutions, Animals, Sampling, Sample analysis, Pharmacokinetic and statistical analysis; Results: BNP7787 administration and BNP7787 vs mesna administration; Figures 3–4; Discussion (AUC limitations)

BNP7787 · Materials and Methods: Drug solutions, Animals, Sampling, Sample analysis, Pharmacokinetic and statistical analysis; Results: BNP7787 administration and BNP7787 vs mesna administration; Figures 3–4; Discussion (AUC limitations)

Mesna comparator · Materials and Methods: Drug solutions, Animals, Sampling, Sample analysis, Pharmacokinetic and statistical analysis; Results: BNP7787 administration and BNP7787 vs mesna administration; Figures 3–4; Discussion (AUC limitations)

Specifications

Manufacturer Adooq Bioscience
CAS Number 16208-51-8
Applications Protective agent
Formula C4H8Na2O6S4
Molecular Weight 326.3
Synonyms Tavocept; BioNumerik; BNP7787
SMILES
C(CS(=O)(=O)[O-])SSCCS(=O)(=O)[O-].[Na+].[Na+]

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

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] Parker AR, Nienaber VL, Petluru PN, et al. BNP7787 Forms Novel Covalent Adducts on Human Thioredoxin and Modulates Thioredoxin Activity Journal of Pharmacology & Clinical Toxicology (2014). Source material
  2. [2] Parker AR, Petluru PN, Nienaber VL, et al. Cysteine specific targeting of the functionally distinct peroxiredoxin and glutaredoxin proteins by the investigational disulfide BNP7787. Molecules (Basel, Switzerland) (2015). PMID: 25793542 DOI: 10.3390/molecules20034928 Source material
  3. [3] Verschraagen M, Boven E, Torun E, et al. Pharmacokinetic behaviour of the chemoprotectants BNP7787 and mesna after an i.v. bolus injection in rats. British journal of cancer (2004). PMID: 15083199 DOI: 10.1038/sj.bjc.6601719 Source material

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